Novel compounds having anticancer activity and their production method

Abstract

The present invention relates to a novel compound having anti-cancer activity and a method for preparing the same, more particularly to a novel compound that inhibits the expression of AIMP2-DX2 and exhibits excellent anti-cancer activity, and a method for preparing the same. The compound represented by Chemical Formula 1 according to the present invention has an excellent effect of inhibiting the expression of AIMP2-DX2, and can be very useful in developing therapeutic agents for various diseases induced by AIMP2-DX2, particularly cancer.

Description

[Technical field]

[0001] This application claims priority based on Korean Patent Application No. 10-2019-0037271, filed on March 29, 2019, the entire specification of which is incorporated herein by reference.

[0002] The present invention relates to a novel compound having anticancer activity and a method for producing the same, and more particularly to a novel compound that suppresses the expression of AIMP2-DX2 and exhibits excellent anticancer activity, and a method for producing the same. [Background technology]

[0003] AIMP2 (aminoacyl-tRNA synthetase complex-interacting multifunctional protein 2) is one of the proteins involved in the formation of aminoacyl-tRNA synthetase (ARS) complexes. In addition to its essential function in protein synthesis, AIMP2 is known to function as a novel tumor suppressor by enhancing TGF-β signaling through direct interaction with Smad2 / 3.

[0004] As disclosed in Patent Document 1 by the present inventor, AIMP2-DX2, a mutant form in which exon 2 of AIMP2 is deleted, was observed to be overexpressed in various cancer cell lines and tissues, such as lung cancer, liver cancer, skin cancer, breast cancer, kidney cancer, and osteosarcoma. Meanwhile, it was confirmed that when normal cells were transformed to overexpress AIMP2-DX2, the wild-type (WT) AIMP2 level was significantly reduced, and the activity of AIMP2 was suppressed, such as preventing AIMP2 from migrating to the nucleus, leading to functional abnormalities of TGF-β signaling, such as increased c-myc expression and promotion of cell growth. This indicates that there is a close relationship between AIMP2-DX2 and the occurrence and progression of cancer. In addition, the present inventor's other patent document 2 disclosed for the first time that AIMP2 mediates the apoptotic activity of TNF-α through interaction with TRAF2, and that this activity is regulated by AIMP2-DX2. It was also revealed that AIMP2-DX2 also affects the expression of COX-2, an inflammatory marker, and it was proposed that the therapeutic effect of inflammatory diseases can be achieved by suppressing the activity of AIMP2-DX2.

[0005] As described above, it has become clear that the AIMP2-DX2 protein is involved in the induction and progression of various diseases, making AIMP2-DX2 a new target substance for the development of new drugs. [Prior art documents] [Patent documents]

[0006] [Patent Document 1] Korean Patent No. 10-0762995 [Patent Document 2] Korean Patent No. 10-1067816 Summary of the Invention [Problem to be solved by the invention]

[0007] [Detailed Description of the Invention] [Technical issues] Here, the present inventors have conducted extensive research to develop a novel compound capable of inhibiting the expression of AIMP2-DX2, which is closely related to various diseases, and have discovered that the compound represented by Chemical Formula 1 herein inhibits the expression of AIMP2-DX2 and exhibits excellent anti-cancer activity, thereby completing the present invention. Accordingly, an object of the present invention is to provide a compound represented by the following Chemical Formula 1 or a pharma- ceutically acceptable salt thereof. [Chemical formula 1] [ka] In the above Chemical Formula 1, R1 is hydrogen; C1-C5 straight or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; C1-C5 carboxymethyl; C7-C10 hydroxyphenylalkyl; substituted or unsubstituted C3-C8 cycloalkyl; substituted or unsubstituted C1-C5 aminoalkyl; [ka] Or, [ka] and R2 is hydrogen; benzenesulfonyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, a nitro group, an amine group, halo, -CF3, C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH2Ph, hydroxy, -COOCH2Ph, C1-C5 alkyloxycarbonyl, -CONHCH3, and nitrile; naphthalenesulfonyl; benzylsulfonyl; benzoyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, and C1-C5 linear or branched alkylamine groups; thiophenesulfonyl; [ka] ; [ka] ; [ka] ; C1-C5 alkyloxycarbonyl; or phenylaminocarbonyl, R3 is, [ka] [ka] [ka] [ka] [ka] [ka] or [ka] It is.

[0008] Another object of the present invention is to provide a pharmaceutical composition for preventing or treating cancer, comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient. Another object of the present invention is to provide a pharmaceutical composition for preventing or treating cancer, comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient. Another object of the present invention is to provide a pharmaceutical composition for preventing or treating cancer, which essentially consists of the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient.

[0009] It is yet another object of the present invention to provide a use of the compound of Formula 1 or a pharma- ceutically acceptable salt thereof for the manufacture of a preparation for the prophylaxis or treatment of cancer. It is yet another object of the present invention to provide a method for treating cancer, comprising administering an effective amount of a composition comprising the compound of Chemical Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient to an individual in need thereof. It is still another object of the present invention to provide a use of the compound of formula 1 or a pharma- ceutically acceptable salt thereof for the manufacture of a preparation for the prophylaxis or treatment of an inflammatory disease. It is yet another object of the present invention to provide a method for treating an inflammatory disease, comprising administering an effective amount of a composition comprising the compound of Formula 1 or a pharma- ceutical acceptable salt thereof as an active ingredient to an individual in need thereof. [Means for solving the problem]

[0010] In order to achieve the above object of the present invention, the present invention provides a compound represented by the following formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] [ka] In the above Chemical Formula 1, R1 is hydrogen; C1-C5 straight or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; C1-C5 carboxymethyl; C7-C10 hydroxyphenylalkyl; substituted or unsubstituted C3-C8 cycloalkyl; substituted or unsubstituted C1-C5 aminoalkyl; [ka] Or, [ka] and R2 is hydrogen; benzenesulfonyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, a nitro group, an amine group, halo, -CF3, C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH2Ph, hydroxy, -COOCH2Ph, C1-C5 alkyloxycarbonyl, -CONHCH3, and nitrile; naphthalenesulfonyl; benzylsulfonyl; benzoyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, and C1-C5 linear or branched alkylamine groups; thiophenesulfonyl; [ka] ; [ka] ; [ka] ; C1-C5 alkyloxycarbonyl; or phenylaminocarbonyl, R3 is, [ka] [ka] [ka] [ka] [ka] [ka] Or, [ka] It is.

[0011] In order to achieve another object of the present invention, there is provided a pharmaceutical composition comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient. In addition, there is provided a pharmaceutical composition for preventing or treating cancer, comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient. In addition, there is provided a pharmaceutical composition for preventing or treating cancer, which essentially consists of the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient.

[0012] In order to achieve still another object of the present invention, there is provided a use of the compound of formula 1 or a pharma- ceutically acceptable salt thereof for manufacturing a preparation for preventing or treating cancer.In order to achieve still another object of the present invention, there is provided a method for treating cancer, comprising administering an effective amount of a composition comprising the compound of formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient to an individual in need thereof. In order to achieve yet another object of the present invention, there is provided a use of the compound of Formula 1 or a pharma- ceutically acceptable salt thereof for preparing a preparation for preventing or treating an inflammatory disease. In order to achieve yet another object of the present invention, there is provided a method for treating an inflammatory disease, comprising administering an effective amount of a composition containing the compound of Formula 1 or a pharma- ceutical acceptable salt thereof as an active ingredient to an individual in need thereof.

[0013] The present invention will be described in detail below. The present invention provides a compound represented by the following formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] [ka] In the above Chemical Formula 1, R1 is hydrogen; C1-C5 straight or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; C1-C5 carboxymethyl; C7-C10 hydroxyphenylalkyl; substituted or unsubstituted C3-C8 cycloalkyl; substituted or unsubstituted C1-C5 aminoalkyl; [ka] Or, [ka] and R2 is hydrogen; benzenesulfonyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, a nitro group, an amine group, halo, -CF3, C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH2Ph, hydroxy, -COOCH2Ph, C1-C5 alkyloxycarbonyl, -CONHCH3, and nitrile; naphthalenesulfonyl; benzylsulfonyl; benzoyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, and C1-C5 linear or branched alkylamine groups; thiophenesulfonyl; [ka] ; [ka] ; [ka] ; C1-C5 alkyloxycarbonyl; or phenylaminocarbonyl, R3 is, [ka] [ka] [ka] [ka] [ka] [ka] Or, [ka] It is.

[0014] In the present invention, the term "alkyl" refers to a straight or branched aliphatic hydrocarbon group containing 1 to 5 carbon atoms in the chain. Preferred alkyl groups contain 1 to 3 carbon atoms in the chain. More preferred alkyl groups contain about 1, 2 or 3 carbon atoms in the chain. Branched means that one or more lower alkyl groups, e.g., methyl, ethyl, or propyl, are attached to a linear alkyl chain. "Lower alkyl" refers to a group having 1 to 5 carbon atoms in the chain, which may be straight or branched. "Alkyl" may be unsubstituted or may be optionally substituted with one or more substituents, which may be the same or different.

[0015] In the present invention, the term "halo" or "halogen" refers to a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom.

[0016] When a group disclosed in the present invention is expressed as "substituted", the group may be substituted with any suitable substituent or substituent. Illustrative examples of the substituents include those that can be confirmed through the exemplary compounds and specific examples disclosed in the present invention, as well as halogen (chloro, iodine, bromo or fluorine groups), alkyl, hydroxyl, alkoxy, alkoxyalkyl, amino, alkylamino, carboxy, nitro, ano, thiol, thioether, imine, imide, amidine, guanidine, enamine, aminocarbonyl, acylamino, phosphonate, phosphine, thiocarbonyl, sulfonyl, sulfone, sulfonamide, ketone, aldehyde, ester, urea, urethane, oxime, hydroxylamine, alkoxyamine, aralkoxyamine, N-oxide, hydrazine, hydrazide, hydrazone, azide, isocyanate, isothiocyanate, cyanate, thiocyanate, etc.

[0017] In one aspect of the present invention, R1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl, R2 is an unsubstituted or substituted benzenesulfonyl group selected from the group consisting of C1 to C5 linear or branched alkyl, a nitro group, an amine group, halo, -CF3, C1 to C5 alkylcarbonylamino, -COOH, C1 to C5 alkoxy, phenyl, -OCH2Ph, hydroxy, -COOCH2Ph, C1 to C5 alkyloxycarbonyl, -CONHCH3, and nitrile; The R3 is [ka] or [ka] That's fine too.

[0018] Preferably, R1 is an unsubstituted C1-C5 linear or branched alkyl; or an unsubstituted indolylmethyl; R2 is a benzenesulfonyl group which may be unsubstituted or substituted with a C1-C5 linear or branched alkyl group; The R3 is [ka] or [ka] That's fine too.

[0019] In another embodiment of the present invention, R1 is preferably hydrogen, cyclohexane, [ka] or [ka] That's fine too.

[0020] In another embodiment of the present invention, R1 is most preferably [ka] Or, [ka] That's fine too.

[0021] In another embodiment of the invention, R2 is preferably hydrogen, [ka] Or, [ka] That's fine too.

[0022] In another embodiment of the present invention, R3 is preferably [ka] [ka] [ka] Or, [ka] That's fine too.

[0023] In addition, in the present invention, the compound of Chemical Formula 1 is (S)-4-methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (R)-4-methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (S)-4-methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (R)-4-methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)-pentan-2-yl)benzenesulfonamide, (S)-N-(1-(1,1-dioxidothiomorpholino)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide, N-((S)-1-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(piperidin-1-yl)phenyl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-methylpiperidin-1-yl)phenyl)pentanamide, (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyridin-3-yl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyrimidin-4-yl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide, (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)pentanamide, (S)-N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-N-(3-fluoro-4-morpholinophenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-N-(4-(1,1-dioxidothiomorpholino)phenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-tert-butyl 4-(5-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido)pyridin-2-yl)piperazine-1-carboxylate, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(pyrrolidin-1-yl)phenyl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(2-morpholinoethyl)pentanamide, (S)-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-nitrobenzenesulfonamide, (S)-3-amino-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (S)-2-(4-fluorophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-2-(4-bromophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(3-nitrophenylsulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(naphthalene-1-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(naphthalene-2-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(phenylsulfonamido)pentanamide, (S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate, (S)-2-(4-methoxyphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(thiophene-2-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)pentanamide, (S)-2-(4-isopropylphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-2-(biphenyl-4-ylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-(benzyloxy)-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (S)-4-hydroxy-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (S)-benzyl 4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoate, (S)-tert-butyl 3-(4-methylphenylsulfonamido)-4-morpholino-4-oxobutanoate, (S)-4-methyl-N-(1-morpholino-1-oxo-3-phenylpropan-2-yl)benzenesulfonamide, (S)-N-(3-hydroxy-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-4-methyl-N-(3-methyl-1-morpholino-1-oxobutan-2-yl)benzenesulfonamide, (R)-N-(3-mercapto-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (2S,3S)-3-hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide, (2S,3S)-3-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-2-(4-methylphenylsulfonamido)-4-(methylthio)-N-(4-morpholinophenyl)butanamide, (S)-3-(1H-indol-2-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1-methyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide, (S)-benzyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate, (S)-benzyl 4-methyl-2-(4-methylbenzamido)pentanoate, (S)-benzyl 2-(4-tert-butylbenzamido)-4-methylpentanoate, (S)-benzyl 2-(benzo [d] [1,3] dioxole-5-carboxamido)-4-methylpentanoate, (S)-benzyl 2-(4-(tert-butoxycarbonylamino)benzamido)-4-methylpentanoate, (S)-benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate, (S)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-1-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-phenylurea, (S)-4-tert-butyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzamide, (S)-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-(phenylsulfonyl)propanamide, (S)-4-tert-butyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide, (S)-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzo[d][1,3]dioxole-5-carboxamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(3-(phenylsulfonyl)propanamido)pentanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(2-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(3-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-2-(3,5-dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfon-amido)propanamide, (S)-3-(5-Hydroxy-1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)propan amide, (S)-2-(2,4-dimethylphenylsulfonamido)-3-(1 H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, 3-(3-ethoxy-2-(4-methylphenylsulfonamido)-3-oxopropyl)-1 H-indole-5-carboxylic acid, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(1-tosyl-1 H-imidazol-4-yl)propanamide, (S)-N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (R)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-N-(3-fluoro-4-morpholinophenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methoxyphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4 morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propenamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide, (S)-N-(benzo [d] thiazol-2-yl)-3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanoic acid, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)pentanamide, (S)-N-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-N-(5-(4-methoxyphenyl)isoxazol-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)pentanamide, (S)-N-(4-(3,4-dimethoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-N-(4-(2-bromo-4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-(2-aminothiazol-4-yl)phenyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate, (S)-N-(4-(4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethoxy)phenyl)thiazol-2-yl)pentanamide, (S)-N-(4-(4-hydroxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-p-tolylthiazol-2-yl)pentanamide, (S)-N-(4-(4-((S)-1-methoxypropan-2-yloxy)phenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)pentanamide, (S)-methyl 4-(2-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido)thiazol-4-yl)benzoate, (S)-4-(2-(4-methylphenylsulfonamido)-3-(4-morpholinophenylamino)-3-oxopropyl)phenyl 4-methylbenzenesulfonate, (S)-2-(4-bromophenylsulfonamido)-3-(1H-imidazol-4-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-N-methoxy-N,4-dimethyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-3-(1H-indol-3-yl)-N-methoxy-N-methyl-2-(4-methylphenylsulfonamido)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)propan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-tert-butylphenylsulfonamido)-3-(1 H-indol-3-yl)-N-(4-morpholinophenyl)propan amide, (S)-2-(4-bromophenylsulfonamido)-N-(4-(2-chlorophenyl)thiazol-2-yl)-3-(1 H-indol-3-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-N-(4-(2,4-dimethoxyphenyl)thiazol-2-yl)-3-(1 H-indol-3-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiazol-2-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(5-methylthiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-methylthiazol-2-yl)propanamide, (S)-methyl 4-(N-(3-(1 H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate, (S)-ethyl 4-(N-(3-(1 H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate, (S)-3-(4-benzoylphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)-N-methylbenzamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(naphthalen-2-yl)propanamide, (S)-tert-butyl 3-(1 H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-ylcarbamate, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoic acid, (S)-tert-butyl 4-(4-(3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-methoxyphenyl)piperazine-1-carboxylate, (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4(piperazin-1-yl)phenyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-tert-butyl 4-(4-(3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)phenyl)piperazine-1-carboxylate, (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-morpholinophenyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(piperazin-1-yl)phenyl)propanamide, (S)-3-(1-formyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-benzyl 3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoate, (S)-benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate, (S)-N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)-4-methylbenzamide, (S)-3-hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide, (S)-1-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-3-phenylurea, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(2-morpholinopyrimidin-5-yl)propanamide, (S)-2-(4-cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanamide, (S)-methyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate, (S)-3-(1H-benzo[d]imidazol-1-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (R)-3-(2,3-dioxo-3,4-dihydroquinoxalin-1(2H)-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)-5-(trifluoromethyl)picolinamide, (S)-benzyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate, (S)-benzyl 3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoate, (S)-4-methyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide, 2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)acetamide, (S)-3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoic acid, (S)-4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoic acid, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenylpropanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenylpropanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(thiophen-2-ylmethyl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiophen-2-ylmethyl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(2-methoxyphenyl)thiazol-2-yl)propanamide, (S)-N-(3-(N-(4-methyl-1-morpholino-1-oxopentan-2-yl)sulfamoyl)phenyl)acetamide, (S)-Benzyl 4-methyl-2-(3-phenylureido)pentanoate, 4-Methyl-N-(2-morpholino-2-oxoethyl)benzenesulfonamide, 4-Methyl-N-(1-(morpholine-4-carbonyl)cyclohexyl)benzenesulfonamide, (S)-4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoic acid, (S)-2-(4-Hydroxyphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoic acid, (S)-2-Amino-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-N-(4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)-3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-N-(4-(4-Acetylpiperazin-1-yl)phenyl)-3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-morpholinobenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)propanamide, (S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate, (S)-Benzyl 3-(1 H-indol-3-yl)-2-(6(trifluoromethyl)pyridine-3-sulfonamido)propanoate, (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5 -(4-Nitrophenyl)pentanediamide ((S)-2-(4-Methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)-N 5 -(4-nitrophenyl)pentanediamide), (S)-Benzyl 5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexylcarbamate, (S)-6-Amino-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)hexanamide, (S)-3,5-Dimethoxy-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)benzamide, (S)-N 5 -(4-Methoxybenzyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide ((S)-N 5-(4-Methoxybenzyl)-2-(4-methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)pentanediamide), (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5 -Phenylpentanediamide ((S)-2-(4-Methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)-N 5 -phenylpentanediamide), (S)-2-(4-Methylphenylsulfonamido)-5-morpholino-N-(4-morpholinophenyl)-5-oxopentanamide, (S)-N 5 -(4-fluorophenyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide ((S)-N 5 -(4-fluorophenyl)-2-(4-methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)pentanediamide), (S)-N 5 -(4-tert-butylphenyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide ((S)-N 5 -(4-tert-butylphenyl)-2-(4-methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)pentanediamide), (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5-(4-(trifluoromethyl)phenyl)pentanediamide ((S)-2-(4-Methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)-N 5 -(4-(trifluoromethyl)phenyl)pentanediamide), (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 4 -(4-Nitrophenyl)succinic acid amide ((S)-2-(4-Methylphenylsulfonamido)-N 1 -(4-morpholinophenyl)-N 4 -(4-nitrophenyl)succinamide), (S)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-isopropyl-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-isopropylpropanamide, (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoyl)-N-(4-methoxyphenyl)hydrazinecarboxamide, (S)-4-Bromo-N-(1-(3,5-dimethyl-1 H-pyrazol-1-yl)-3-(1 H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)-N-(3-(1H-indol-3-yl)-1-oxo-1-(3-phenyl-1H-pyrazol-1-yl)propan-2-yl)-4-bromobenzenesulfonamide, N-((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(p-tolyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenethylpropanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-fluorophenyl)thiazol-2-yl)-3-(1 H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-nitrophenyl)thiazol-2-yl)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-cyanophenyl)thiazol-2-yl)-3-(1 H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide, (S)-4-Bromo-N-(1-(2-dodecanoylhydrazinyl)-3-(1 H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)-4-Bromo-N-(1-(2-decanoylhydrazinyl)-3-(1 H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenethylpropanamide, N-((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-fluorophenethyl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(3-phenylpropyl)propanamide, (S)-N-((3R,5R,7R)-adamantan-1-yl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide, (S)-N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl) piperazin-1-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-N-((3R,5R,7R)-adamantan-1-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(3-phenylpropyl)propanamide, (S)-N-(4-fluorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide, (S)-N-(2-(1H-indol-3-yl)ethyl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide, (S)-N-(3-(1H-indol-3-yl)-1-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-1-oxopropan-2-yl)-4-methylbenzamide, (S)-2-(4-Chlorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-(trifluoromethyl)phenylsulfonamido)propanamide, (S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-((1r,3R,5S,7S)-3,5-dimethyladamantan-1-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate, (S)-2-(4-Bromophenylsulfonamido)-3-(5-hydroxy-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-3-(5-methyl-1 H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(5-fluoro-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)ethyl)benzoic acid, (S)-N-(4-bromophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-N-(2-(1H-indol-3-yl)ethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-methylphenethyl)-2-(4-methylphenylsulfonamido)propanamide, Ethyl 2-((S)-3-(1 H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1 H-indol-3-yl)propanoate, (S)-N-(4-chlorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoic acid, (S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate, (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoic acid, (S)-3-(Benzo[d]oxazol-2-ylamino)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)benzamide, (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)nicotinamide, or (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)pyrimidine-5-carboxamide That's fine too.

[0024] The structural formulas of the compounds, the inhibitory effects of these compounds on AIMP2-DX2 expression, and the cytotoxicity of these compounds against cancer cells are shown in Table 1 below. [Table 1] [Table 1] [Table 2] [Table 3] [Table 4] [Table 5] [Table 6] [Table 7]

Table 8

Table 9

Table 10

Table 11

Table 12

Table 13

Table 14

Table 15

Table 16

Table 17

Table 18

Table 19

Table 20

Table 21

[0025] The compound of the present invention represented by Chemical Formula 1 can be used in the form of a pharma- ceutically acceptable salt. As the salt, acid addition salts formed with various pharma- ceutically or physiologically acceptable organic or inorganic acids are useful. Suitable organic acids include, for example, carboxylic acid, phosphonic acid, sulfonic acid, acetic acid, propionic acid, octanoic acid, decanoic acid, glycolic acid, lactic acid, fumaric acid, succinic acid, adipic acid, malic acid, tartaric acid, citric acid, glutamic acid, aspartic acid, maleic acid, benzoic acid, salicylic acid, phthalic acid, phenylacetic acid, benzenesulfonic acid, 2-naphthalenesulfonic acid, methylsulfuric acid, ethylsulfuric acid, dodecylsulfuric acid, etc., and suitable inorganic acids include, for example, hydrochloric acid, sulfuric acid, or phosphoric acid.

[0026] The compound of the present invention represented by Chemical Formula 1 may include, in addition to pharma- ceutically acceptable salts, all salts, hydrates and solvates, racemates, or stereoisomers that can be prepared by conventional methods.

[0027] In one embodiment of the present invention, the compound was confirmed to exhibit an activity of inhibiting the expression of AIMP2-DX2, and in particular, it was confirmed that such activity is exerted by inhibiting the binding of AIMP2-DX2 protein to HSP70, which contributes to the stabilization of the protein. Therefore, the compounds provided by the present invention can be characterized as exhibiting activity of suppressing the expression of AIMP2-DX2.

[0028] The present invention also provides a method for preparing the compound of claim 1 or a pharma- ceutically acceptable salt thereof, which is prepared according to the following reaction scheme: [Reaction Scheme 1] [ka]

[0029] In the reaction scheme 1, R1, R2 and R3 are as defined above.

[0030] Meanwhile, in one embodiment of the present invention, the compound of Chemical Formula 1 or a pharma- ceutically acceptable salt thereof was confirmed to inhibit the expression of AIMP2-DX2, exhibit excellent cytotoxicity against cancer cells, and exhibit an extremely excellent effect of inhibiting tumor growth in an in vivo tumor model. Therefore, the present invention provides a pharmaceutical composition for preventing or treating cancer, comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient.

[0031] On the other hand, according to previous reports, it has been confirmed that inhibiting the expression of AIMP2-DX2 suppresses the expression of COX-2 and alleviates inflammatory reactions (Korean Patent No. 1067816). Therefore, the compound of the present invention that inhibits the expression of AIMP2-DX2 can also show excellent activity against inflammatory diseases.

[0032] Here, the present invention provides a pharmaceutical composition for preventing or treating an inflammatory disease, comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient. In the present invention, the inflammatory disease includes inflammatory skin diseases, Crohn's disease, ulcerative colitis, peritonitis, osteomyelitis, cellulitis, meningitis, encephalitis, pancreatitis, trauma-induced shock, bronchial asthma, allergic rhinitis, cystic fibrosis, stroke, acute bronchitis, chronic bronchitis, acute bronchiolitis, chronic bronchiolitis, osteoarthritis, gout, spondyloarthropathy, ankylosing spondylitis, Reiter's syndrome, psoriatic arthropathy, enteropathic spondylitis, juvenile arthropathy, juvenile ankylosing spondylitis, reactive arthropathy, infectious arthropathy, and the like. Arthritis, post-infectious arthritis, gonococcal arthritis, tuberculous arthritis, viral arthritis, fungal arthritis, syphilitic arthritis, Lyme disease, arthritis associated with the "vasculitis syndrome", polyarteritis nodosa, hypersensitivity vasculitis, Lou Gehrig's granulomatosis, polymyalgia rheumatica, arthrocyte arthritis, calcium crystal deposition arthropathy, pseudogout, non-articular rheumatoid arthritis, mucositis, tenosynovitis, epicondylitis (tennis elbow), neuropathic joint disease (charco and joint, hemarthrosic, Henoch-Schönlein purpura, hypertrophic osteoarthropathy, multicentric reticulohistiocytosis, sarcoilosis, hemochromatosis, sickle cell disease and other hemochromatoses, hyperlipoproteinemia, hypogammaglobulinemia, familial Mediterranean fever, Behat's disease, systemic lupus erythematosus, relapsing fever, psoriasis, multiple sclerosis, sepsis, septic shock, multiple organ dysfunction syndrome, acute respiratory distress syndrome, chronic obstructive pulmonary disease, rheumatoid arthritis, acute lung injury and broncho-pulmonary dysplasia.

[0033] The pharmaceutical composition according to the present invention may contain the compound of Formula 1 or a pharma- ceutically acceptable salt thereof alone, or may additionally contain one or more pharma- ceutically acceptable carriers, excipients, or diluents.

[0034] The pharma- ceutically acceptable carrier may further include, for example, a carrier for oral administration or a carrier for parenteral administration. The carrier for oral administration may include lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, etc. The carrier for parenteral administration may further include water, suitable oil, saline, aqueous glucose and glycol, etc., and may further include stabilizers and preservatives. Suitable stabilizers include antioxidants such as sodium bisulfite, sodium sulfite, or ascorbic acid. Suitable preservatives include benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol. Other pharma- ceutically acceptable carriers may be referred to those known in the art.

[0035] The pharmaceutical composition of the present invention can be administered to mammals, including humans, by any method. For example, it can be administered orally or parenterally. Parenteral administration methods include, but are not limited to, intravenous, intramuscular, intraarterial, intramedullary, intradural, intracardiac, transdermal, subcutaneous, intraperitoneal, intranasal, intestinal, topical, sublingual, or rectal administration. For example, the pharmaceutical composition of the present invention can be prepared in an injection form and administered by lightly pricking the skin with a 30-gauge thin injection needle or by directly applying to the skin.

[0036] The pharmaceutical composition of the present invention can be formulated as a preparation for oral administration or parenteral administration depending on the administration route as described above.

[0037] In the case of oral preparations, the composition of the present invention may be in the form of powder, granules, tablets, pills, sugar-coated tablets, capsules, liquids, gels, syrups, slurries, suspensions, etc., and may be formulated by methods known in the art. For example, oral preparations may be prepared by blending the active ingredient with a solid excipient, grinding the mixture, adding suitable auxiliary agents, and processing the mixture with a granule to obtain tablets or sugar-coated tablets. Examples of suitable excipients include sugars including lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, and maltitol, starches including corn starch, wheat starch, rice starch, and potato starch, celluloses including cellulose, methylcellulose, sodium carboxymethylcellulose, and hydroxypropylmethyl-cellulose, gelatin, polyvinylpyrrolidone, and other fillers. In addition, cross-linked polyvinylpyrrolidone, agar, alginic acid, or sodium alginate may be added as a disintegrant, if necessary. Furthermore, the pharmaceutical composition of the present invention may additionally contain an anti-coagulant, a lubricant, a wetting agent, a flavoring agent, an emulsifier, a preservative, and the like.

[0038] For parenteral administration, the formulations may be in the form of injections, creams, lotions, topical ointments, oils, moisturizers, gels, aerosols and nasal inhalers, and may be formulated in any manner known in the art, and may be described in formulary forms generally known in all pharmaceutical chemistry.

[0039] The total effective amount of the pharmaceutical composition of the present invention can be administered to a patient in a single dose or in a fractionated treatment protocol in which multiple doses are administered over a long period of time. The pharmaceutical composition of the present invention can vary the content of the active ingredient depending on the severity of the disease. Preferably, the total amount of the pharmaceutical composition of the present invention can be about 0.01ug to 1,000mg per kg of patient body weight per day, most preferably 0.1ug to 100mg. However, the effective dose of the pharmaceutical composition of the present invention is determined by taking into consideration various factors such as the age, body weight, health condition, sex, severity of the disease, diet, and excretion rate of the patient, as well as the administration route and number of treatments. Taking this into consideration, a person having ordinary knowledge in the art can determine an appropriate effective dose of the pharmaceutical composition of the present invention according to a specific use as a therapeutic agent for degenerative neurological diseases. The pharmaceutical composition of the present invention is not particularly limited in its dosage form, administration route, and administration method, as long as it shows the effect of the present invention.

[0040] In the present invention, the term "treatment" comprehensively refers to improving the symptoms of cancer or inflammatory disease, which may preferably include curing, substantially preventing, or improving the condition of cancer or inflammatory disease, and includes, but is not limited to, alleviating, curing, or preventing one or most of the symptoms, including cancer or inflammatory disease.

[0041] The present invention provides use of the compound of Formula 1 or a pharma- ceutically acceptable salt thereof for the manufacture of a preparation for the prophylaxis or treatment of cancer. The present invention provides a method for treating cancer, comprising administering an effective amount of a composition comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient to an individual in need thereof. The present invention provides use of the compound of formula 1 or a pharma- ceutically acceptable salt thereof for the manufacture of a preparation for the prophylaxis or treatment of an inflammatory disease. The present invention provides a method for treating an inflammatory disease, comprising administering an effective amount of a composition comprising the compound of Formula 1 or a pharma- ceutically acceptable salt thereof as an active ingredient to an individual in need thereof.

[0042] The "effective amount" of the present invention refers to an amount that shows an effect of improving, treating, preventing, detecting, diagnosing, or suppressing or reducing cancer or inflammatory disease when administered to an individual, and the "individual" may be an animal, preferably a mammal, particularly an animal including a human, or a cell, tissue, organ, etc. derived from an animal. The individual may be a patient in need of the effect.

[0043] In this specification, the term "comprising" is used interchangeably with "including" or "characterized by" and does not exclude additional components or method steps not specifically mentioned in the composition or method of the present invention. The term "consisting of" means excluding additional elements, steps, ingredients, etc. not otherwise described. The term "essentially consisting of" means that the scope of the composition or method can include, in addition to the substances or steps described, substances or steps that do not substantially affect its basic characteristics. Effect of the Invention

[0044] The compound represented by Chemical Formula 1 according to the present invention has an excellent effect of inhibiting the expression of AIMP2-DX2, and can be very usefully used in the development of therapeutic agents for various diseases induced by AIMP2-DX2, especially cancer. [Brief description of the drawings]

[0045] [Figure 1]FIG. 1 shows the results of measuring the fluorescence after treating A549 cells expressing nanoluciferase-DX2 or AIMP2 with compound 63 (compound No. 63) of the present invention at different concentrations for 4 hours, and calculating the IC50 of AIMP2-DX2 and AIMP2. [Diagram 2] Figure 2 shows the results of in vitro pull-down assay confirming that compound 63 of the present invention inhibits the binding of AIMP2-DX2 to HSP70. Purified AIMP2-DX2-His6 and HSP70 proteins were mixed and treated with compound 63 at different concentrations for 4 hours, after which AIMP2-DX2 was precipitated with Ni-IDA resin, and HSP70 precipitated together with AIMP2-DX2 was visualized by SDS-PAGE and Coomassie staining. [Figure 3a] Figure 3a shows the results of administering compound 63 (50 mg / kg) intraperitoneally to mice implanted with H460 cells once every two days for a total of 15 days, and observing the growth of the tumor (Figure 3a: macroscopic observation of each mouse and tumor after completion of administration). [Figure 3b] Figure 3b shows the results of administering compound 63 (50 mg / kg) intraperitoneally to mice implanted with H460 cells once every two days for a total of 15 days, and observing tumor growth (Figure 3b: tumor growth curve over time). [Figure 3c] Figure 3c shows the results of administering compound 63 (50 mg / kg) intraperitoneally to mice implanted with H460 cells once every two days for a total of 15 days, and observing the growth of the tumor (Figure 3c: weight of each tumor obtained at the end of administration). [Figure 3d] Figure 3d shows the results of administering compound 63 (50 mg / kg) intraperitoneally to mice implanted with H460 cells once every two days for a total of 15 days, and observing the growth of the tumor (Figure 3d: change in animal weight during the administration period). [Figure 4]4 shows the results of testing the cancer cell growth inhibitory effect and tumor distribution of compound 55 (compound no. 55) and compound 89 (compound no. 89) among the compounds of Formula 1 according to the present invention in an H460 xenograft animal model. Taxol was used as a positive control. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0046] The present invention will be described in detail below. However, the following examples are merely illustrative of the present invention, and the content of the present invention is not limited to the following examples.

[0047] Example 1: Preparation of Compounds In the present invention, the compound of Formula 1 was prepared according to the following Reaction Scheme 1: [Reaction Scheme 1] [ka] In the above reaction scheme, R1, R2 and R3 are as defined above.

[0048] Specifically, starting material acid (1) (1.0 eq.) was prepared in 2M NaOH solution (1.0 eq.). The mixture was stirred at 0°C for several minutes until a clear solution was formed. To the solution was added sulfonyl chloride (1.05 eq.), DIPEA (1.1 eq.) and acetone. The mixture was stirred at 0°C for 10 minutes and then at room temperature for 12 hours. After completion of the reaction, the mixture was washed with ether to remove organic impurities. The combined organic layer was washed again with 2M NaOH. 2N HCl was added to the aqueous layer at 0°C until the pH was 2. The entire aqueous mixture was then extracted with ethyl acetate, water and brine. The organic solvent was dried over MgSO4 and evaporated in vacuum to obtain compound (2). To 15 mL of DMF or DCM:THF=1:1, compound (2 eq.), amine (1.1 eq.), EDCl (1.1 eq.) and HOBt (1.1 eq.) were added. The mixture was stirred at room temperature overnight and then extracted with ethyl acetate, water and brine. The organic layer was dried over MgSO4 and evaporated in vacuum to obtain crude compound (3), which was purified by column chromatography to obtain pure compound (3).

[0049] Specific examples of the compound of Formula 1 prepared according to the above method, its structure and NMR analysis results are shown below.

[0050] (S)-4-Methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.70(d, J=8.40Hz, 2H), 7.29(d, J=8.00Hz, 2H), 5.74(d, J=9.60Hz, 1H), 4.06-4.01(m, 1H), 3.61-3.51(m, 2H), 3.41-3.36 (m, 1H), 3.31-3.14(m, 5H), 2.42(s, 3H), 2.00-1.93(m, 1H), 1.50-1.43( m, 1H), 1.17-1.11(m, 1H), 0.95(d, J=6.80Hz, 3H), 0.92(d, J=6.80Hz, 3H) (R)-4-Methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.70(d, J=8.80Hz, 2H), 7.29(d, J=8.40Hz, 2H), 5.78(d, J=9.60Hz, 1H), 4.08-4.02(m, 1H), 3.59-3.42(m, 2H), 3.41-3.32 (m, 1H), 3.31-3.15(m, 5H), 2.41(s, 3H), 1.99-1.92(m, 1H), 1.50-1.42( m, 1H), 1.19-1.12(m, 1H), 0.95(d, J=6.80Hz, 3H), 0.92(d, J=6.80Hz, 3H) (S)-4-Methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.71(d, J=8.00Hz, 2H), 7.27(d, J=8.00Hz, 2H), 5.59(d, J=10.0Hz, 1H), 4.25-4.19(m, 1H), 3.78-3. 71(m, 2H), 3.69-3.37(m, 11H), 3.22-3.12(m, 3H), 2.40(s, 3H), 1.98-1.91(m, 1H), 1.49-1.33(m, 2H), 0.91(t, J=6.00Hz, 6H) (R)-4-Methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)-pentan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.71(d, J=8.00Hz, 2H), 7.27(d, J=8.40Hz, 2H), 5.66(d, J=9.60Hz, 1H), 4.26-4.20(m, 1H), 3.79-3.67(m, 2H), 3 .66-3.38(m, 11H), 3.23-3.12(m, 3H), 2.40(s, 3H), 1.97-1.90(m, 1H), 1.49-1.33(m, 2H), 0.92(d, J=4.20Hz, 3H), 0.89(d, J=5.60Hz, 3H) (S)-N-(1-(1,1-dioxidothiomorpholino)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide 1H-NMR (400MHz, CDCl3) δ7.73 (d, J=7.60Hz, 2H), 7.34 (d, J=7.60Hz, 2H), 5.59 (d, J=9.60Hz, 1H), 4.40(d, J=14.0Hz, 1H), 4.05-3.99(m, 1H), 3.81(d, J=14. 8Hz, 1H), 3.66(t, J=12.6Hz, 1H), 3.32(t, J=12.2Hz, 1H), 2.88(t, J=11.2Hz, 2H), 2.61-2.56(m, 1H), 2.50-2.40(m, 4H), 1.97-1.92(m, 1H), 1.52-1.46(m, 1H), 1.22-1.16(m, 1H), 0.93(d, J=6.40Hz, 3H), 0.85(d, J= 6.40Hz, 3H) N-((S)-1-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.70(d, J=8.20Hz, 2H), 7.28(d, J=7.60Hz, 2H), 5.60(d, J=9.60Hz, 1H) , 4.05(dd, J=3.00, 7.40Hz, 1H), 3.97-3.91(m, 1H), 4.06-4.03(m, 1H), 3.97-3.91(m, 1H), 3.63 -3.61(m, 1H), 3.52-3.49(m, 1H), 3.29-3.25(m, 2H), 2.42(s, 3H), 1.94-1.85(m, 2H), 1.77-1.6 8(m, 2H), 1.56-1.47(m, 2H), 1.25-1.19(m, 1H), 0.94(d, J=3.20Hz, 3H), 0.93(d, J=4.00Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(piperidin-1-yl)phenyl)pentanamide 1H-NMR (400MHz, CDCl3) δ7.85(s, 1H), 7.76(d, J=8.00Hz, 2H), 7.22-7.12(m, 4H), 6.82-6.78(m, 2H), 5.48(s, 1H), 3.84 -3.82(m, 1H), 3.07(t, J=5.60Hz, 4H), 2.32(s, 3H), 1.71-1.46(m, 8H), 0.85(d, J=6.00Hz, 3H), 0.72(d, J=5.60Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-methylpiperidin-1-yl)phenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.97(s, 1H), 7.76(d, J=8.00Hz, 2H), 7.21-7.12(m, 4H), 6.81 -6.77(m, 2H), 5.66(d, J=7.60Hz, 1H), 3.88-3.83(m, 1H), 3.56-3.53(m, 2H), 2.65-2. 58(m, 2H), 2.31(s, 3H), 1.73-1.70(m, 2H), 1.62-1.56(m, 2H), 1.50-1.45(m, 2H), 1.3 7-1.25(m, 2H), 0.97(d, J=6.40Hz, 3H), 0.84(d, J=6.00Hz, 3H), 0.71(d, J=5.60Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyridin-3-yl)pentanamide 1H-NMR (400MHz, CDCl3) δ8.21(s, 1H), 7.98(d, J=2.80Hz, 1H), 7.76(d, J=8.40Hz, 2H), 7.48( dd, J=2.80, 8.80Hz, 1H), 7.22(d, J=8.00Hz, 2H), 6.52(d, J=8.80Hz, 1H), 5.85(d, J=8.00Hz, 1H), 4.16-4.11(m, 2H), 3.91-3.86(m, 1H), 2.78-2.72(m, 2H), 2.32(s, 3H), 1.69-1.47(m, 6H) ), 1.23-1.13(m, 2H), 0.95(d, J=6.00Hz, 3H), 0.83(d, J=6.40Hz, 3H), 0.68(d, J=6.40Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyrimidin-4-yl)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.76 (s, 1H), 8.31 (s, 1H), 7.75 (d, J=8.40Hz, 2H), 7.22(d, J=8.40Hz, 3H), 6.21(s, 2H), 4.37(s, 2H), 3.85(s, 1H), 2.90-2.84( m, 2H), 2.31(s, 3H), 1.80-1.60(m, 4H), 1.53-1.1.47(m, 2H), 1.19-1.09(m, 2H), 0.97(d, J=6.80Hz, 3H), 0.82(d, J=6.80Hz, 3H), 0.70(d, J=6.40Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide 1H-NMR (400MHz, CDCl3) δ7.95(s, 1H), 7.76(d, J=8.00Hz, 2H), 7.28-7.16(m, 4H), 6.84-6.71(m, 2H), 5.49(d, J=7.60Hz, 1H), 3.84(t, J= 4.80Hz, 4H), 3.08(t, J=4.80Hz, 4H), 2.33(s, 3H), 1.60-1.58(m, 2H), 1.50-1.46(m, 1H), 0.84(d, J=6.00Hz, 3H), 0.70(d, J=5.60Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.29(s, 1H), 8.04(d, J=2.40Hz, 1H), 7.77(d, J=8.40Hz, 2H ), 7.59 (dd, J=2.80, 9.20Hz, 1H), 7.23 (d, J=8.40Hz, 2H), 6.52 (d, J=8.80Hz, 1H), 5. 90(d, J=8.00Hz, 1H), 3.92-3.86(m, 1H), 3.80(t, J=5.00Hz, 4H), 3.42(t, J=4.60Hz, 4H), 2.34(s, 3H), 1.60-1.48(m, 3H), 0.83(d, J=6.00Hz, 3H), 0.67(d, J=6.00Hz, 3H) (S)-N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1H-NMR (400MHz, CDCl3) δ8.03(d, J=2.40Hz, 2H), 8.00(s, 1H), 7.77(d, J=8.40Hz, 2H), 7.61(dd, J=2.80, 9. 20Hz, 1H), 7.26(d, J=8.00Hz, 2H), 6.53(d, J=9.20Hz, 1H), 5.48(d, J=7.60Hz, 1H), 4.13(q, J=7.20Hz, 1H) , 3.95(dd, J=2.00, 12.8Hz, 2H), 3.87-3.82(m, 1H), 3.72-3.68(m, 2H), 2.49-2.44(m, 2H), 2.35(s, 3H), 1. 63-1.58(m, 2H), 1.52-1.47(m, 1H), 1.25(d, J=8.00Hz, 6H), 0.85(d, J=6.00Hz, 3H), 0.69(d, J=6.40Hz, 3H) (S)-N-(3-fluoro-4-morpholinophenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.81(s, 1H), 7.76(d, J=8.00Hz, 2H), 7.29(d, J=8.00Hz, 2H), 7.26-7.21(m, 1H), 6.98(d, J=6.00Hz, 1H), 6.85(t, J=9.00Hz, 1H), 4.90(d, J=7.20Hz, 1H), 3.86(t, J=4.60Hz, 4H), 3.77-3.72(m, 1H), 3.04(t, J=4.40Hz, 4H ), 2.38(s, 3H), 1.67-1.43(m, 3H), 0.86(d, J=6.40Hz, 3H), 0.68(d, J=6.40Hz, 3H) (S)-N-(4-(1,1-dioxidothiomorpholino)phenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1H-NMR (400MHz, CDCl3) δ8.07(s, 1H), 7.78(d, J=8.40Hz, 2H), 7.33(d, J=9.20Hz, 2H), 7.28(d, J=8.40Hz, 2H), 6.84(d, J=8.40Hz, 2H), 5.31( d, J=7.20Hz, 1H), 3.82-3.76(m, 5H), 3.10(t, J=5.20Hz, 4H), 2.37(s, 3H), 1.67-1.45(m, 3H), 0.84(d, J=6.40Hz, 3H), 0.65(d, J=6.40Hz, 3H) (S)-Tartyl 4-(5-(4-methyl-2-(4-methylphenylsulfonamido)pentanoyl)pyridin-2-yl)piperazine-1-carboxylate 1 H-NMR (400MHz, CDCl3) δ8.15(s, 1H), 8.02(d, J=2.80Hz, 1H), 7.77(d, J=8.40Hz, 2H), 7.6(dd, J=2.80, 9.20Hz, 1H), 7.25(d, J=8.40Hz, 2H), 6.55(d, J=9.20Hz, 2H) , 5.58(d, J=8.00Hz, 1H), 3.89-3.84(m, 1H), 3.53-3.43(m, 8H), 2.33(s, 3H), 1.62 -1.59(m, 2H), 1.52-1.48(m, 10H), 0.85(d, J=5.60Hz, 3H), 0.69(d, J=6.00Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(pyrrolidin-1-yl)phenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.76(d, J=8.00Hz, 2H), 7.71(s, 1H), 7.23(d, J=8.00Hz, 2H), 7.08-7.04(m, 2H), 6.43-6.39(m, 2H), 5.47(d, J=7.60Hz, 1 H), 3.85-3.79(m, 1H), 3.22(t, J=6.40Hz, 4H), 2.43(s, 3H), 2.03-1.96( m, 4H), 1.64-1.47(m, 3H), 0.86(d, J=6.40Hz, 3H), 0.74(d, J=6.40Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(2-morpholinoethyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.76-7.73(m, 2H), 7.29(d, J=8.00Hz, 2H), 6.65(t, J=4.80Hz, 1H), 5.50(d, J=7.20Hz, 1H), 3.71-3.63(m, 5H), 3.2 9-3.23(m, 1H), 3.18-3.11(m, 1H), 2.46-2.37(m, 9H), 1.57-1.50(m, 2H), 1.44-1.39(m, 1H), 0.83(d, J=6.40Hz, 3H), 0.67(d, J=6.00Hz, 3H) (S)-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-nitrobenzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ8.62 (t, J=2.00Hz, 1H), 8.43-8.40 (m, 1H), 8.17-8.14 (m, 1H), 7.73(t, J=8.00Hz, 1H), 5.82(d, J=10.0Hz, 1H), 4.28-4.22(m, 1H), 3.6 6-3.58(m, 1H), 3.57-3.51(m, 2H), 3.39-3.21(m, 5H), 1.97-1.90(m, 1H), 1.53- 1.45(m, 1H), 1.25-1.18(m, 1H), 0.98(d, J=6.80Hz, 3H), 0.94(d, J=6.40Hz, 3H) (S)-3-Amino-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide 1H-NMR (400MHz, CDCl3) δ7.23(t, J=7.80Hz, 1H), 7.14-7.09(m, 2H), 6.80(dd, J=1.40, 7.80Hz, 1H), 4.11-4.02(m, 3H), 3.61-3.53(m, 2H), 3. 44-3.35(m, 3H), 3.29-3.20(m, 3H), 1.97-1.93(m, 1H), 1.51-1.41(m, 1H), 1.19-1.13(m, 1H), 0.95(d, J=6.00Hz, 3H), 0.91(d, J=6.80Hz, 3H) (S)-2-(4-fluorophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.98(s, 1H), 7.91-7.87(m, 2H), 7.22-7.19(m, 2H), 7.12-7.07(m, 2H), 6.80(dd, J=2.20, 6.60Hz, 2H), 5.74(d, J=7.60) Hz, 1H), 3.85(t, J=5.00Hz, 4H), 3.09(t, J=4.80Hz, 4H), 1.63-1.57(m, 2H), 1.53-1.48(m, 1H), 0.86(d, J=6.40Hz, 3H), 0.73(d, J=6.00Hz, 3H) (S)-2-(4-bromophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.72(d, J=8.40Hz, 2H), 7.59(d, J=8.40Hz, 2H), 7.45(s, 1H), 7 .18(d, J=9.20Hz, 2H), 6.85(d, J=8.80Hz, 2H), 5.19(d, J=8.00Hz, 1H), 3.86(t, J=4.60 Hz, 4H), 3.82-3.77(m, 1H), 3.12(t, J=5.00Hz, 4H), 2.04-1.50(m, 3H), 0.90(d, J=6.40Hz, 3H), 0.8(d, J=5.60Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.99(d, J=8.00Hz, 2H), 7.68(s, 1H), 7.66(d, J=4.00Hz, 2H), 7.10(d, J=12.4Hz, 2H), 6.79(d, J=12.0Hz, 2H), 5.70(d, J=8 .40Hz, 1H), 3.92-3.98(m, 1H), 3.85(t, J=4.80Hz, 4H), 3.09(t, J=4.80H z, 4H), 1.67-1.54(m, 3H), 0.89(d, J=6.00Hz, 3H), 0.79(d, J=6.40Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(3-nitrophenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.70(s, 1H), 8.26(d, J=8.00Hz, 1H), 8.0(d, J=8.20Hz, 1H), 7. 95(s, 1H), 7.61(t, J=8.00Hz, 1H), 7.12(d, J=8.80Hz, 2H), 6.73(d, J=9.20Hz, 2H)), 6. 15(d, J=8.80Hz, 1H), 4.07-4.03(m, 1H), 3.85(t, J=4.60Hz, 4H), 3.08(t, J=4.60Hz, 4H ), 1.72-1.67(m, 1H), 1.60-1.56(m, 2H), 0.90(d, J=6.40Hz, 3H), 0.84(d, J=6.40Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(naphthalene-1-sulfonamido)pentanamide 1H-NMR (400MHz, CDCl3) δ8.82(d, J=8.40Hz, 1H), 8.38(dd, J=0.80, 7.60Hz, 1H), 8.13(s, 1H), 8 .09(d, J=8.00Hz, 1H), 7.99(d, J=8.00Hz, 1H), 7.76-7.65(m, 2H), 7.55(t, J=7.80Hz, 1H), 7.0 9-7.06(m, 2H), 6.79-6.76(m, 2H), 6.07(d, J=7.20Hz, 1H), 3.95-3.90(m, 5H), 3.13(t, J=4.60 Hz, 4H), 1.65-1.61(m, 1H), 1.51-1.44(m, 2H), 0.76(d, J=6.00Hz, 3H), 0.50(d, J=6.80Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(naphthalene-2-sulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.47(s, 1H), 7.96(s, 1H), 7.80-7.81(m, 4H), 7.62-7.52(m, 2H), 7.08-7.05(m, 2H), 6.68-6.64(m, 2H), 5.70(d, J=7.6 0Hz, 1H), 3.97-3.91(m, 1H), 3.83(t, J=4.80Hz, 4H), 3.04(t, J=4.80Hz, 4H), 1.63-1.48(m, 3H), 0.81(d, J=6.40Hz, 3H), 0.63(d, J=5.60Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(phenylsulfonamido)pentanamide 1H-NMR (400MHz, CDCl3) δ7.89(d, J=7.20Hz, 2H), 7.75(s, 1H), 7.56(t, J=7.40H z, 1H), 7.49(t, J=7.40Hz, 2H), 7.24(d, J=9.20Hz, 2H), 6.82(d, J=9.20Hz, 2H), 5.20(d, J=7.20Hz, 2H)), 3.85(t, J=4.80Hz, 4H), 3.81-3.77(m, 1H), 3.10(t, J= 4.80Hz, 4H), 1.66-1.46(m, 3H), 0.85(d, J=6.00Hz, 3H), 0.69(d, J=6.00Hz, 3H) (S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate 1 H-NMR (400MHz, CDCl3) δ7.50(s, 1H), 7.42-7.31(m, 7H), 6.88-6.84(m, 2H), 5.01(d, J=8.000Hz, 1H), 4.27(d, J=3.20Hz, 2H), 3 .86-3.81(m, 5H), 3.12(t, J=4.80Hz, 4H), 1.74-1.60(m, 2H), 1.54-1.47(m, 1H), 0.93(d, J=6.40Hz, 3H), 0.90(d, J=6.40Hz, 3H) (S)-2-(4-methoxyphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.10(s, 1H), 7.83-7.79(m, 2H), 7.26-7.22(m, 2H), 6.89-6.86(m, 2H), 6.80-6.76(m, 2H), 5.60(d, J=7.60Hz, 1H), 3 .87-3.81(m, 5H), 3.76(s, 3H), 3.08(t, J=5.40Hz, 4H), 1.63-1.58(m, 2H), 1.51-1.47(m, 1H), 0.85(d, J=6.00Hz, 3H), 0.70(d, J=5.60Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(thiophene-2-sulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.73(s, 1H), 7.65(dd, J=1.20, 4.00Hz, 1H), 7.58(dd, J=1.20, 4.80Hz, 1H), 7.30-7.27(m, 2H), 7.05(dd, J=3.60, 5.20Hz, 1H), 6.85-6.81(m, 2H), 5.34(s, 1H), 3.91-3.84(m, 5H), 3.11(t, J=5.00H z, 4H), 1.72-1.51(m, 3H), 0.89(d, J=6.00Hz, 3H), 0.79(d, J=6.00Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.23-8.21(m, 2H), 8.03-8.00(m, 2H), 7.12(d, J=8.80Hz, 2H), 6.79(d, J=9.20Hz, 2H), 5.49(d, J=8.80Hz, 1 H), 3.91-3.84(m, 5H), 3.10(t, J=4.80Hz, 4H), 1.76-1.70(m, 1H), 1.61-1.58(m, 3H), 0.93(d, J=6.80Hz, 3H), 0.87(d, J=6.80Hz, 3H) (S)-2-(4-isopropylphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.81-7.78(m, 3H), 7.31(d, J=8.40Hz, 2H), 7.26-7. 21(m, 2H), 6.82-6.78(m, 2H), 5.17(d, J=6.40Hz, 1H), 3.85(t, J=4.00Hz, 4H) , 3.79-3.77(m, 1H), 3.09(t, J=4.80Hz, 4H), 2.94-2.87(m, 1H), 1.68-1.44(m , 3H), 1.19(d, J=6.80Hz, 6H), 0.85(d, J=6.00Hz, 3H), 0.67(d, J=6.00Hz, 3H) (S)-2-(biphenyl-4-ylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.94(d, J=8.20Hz, 2H), 7.87(brs, 1H), 7.59-7.64(m, 2H), 7.37-7.49(m, 5H), 7.15 -7.20(m, 2H), 6.72(d, J=9.00Hz, 2H), 5.48-5.60(m, 1H), 3.87-3.95(m, 1H), 3.79-3.85(m, 4H), 2.98-3.05 (m, 4H), 1.62-1.69(m, 2H), 1.51-1.60(m, 1H), 0.88(d, J=5.80Hz, 3H), 0.76(d, J=5.80Hz, 3H) (S)-4-(Benzyloxy)-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.76-7.73(m, 2H), 7.41-7.32(m, 5H), 7.03-6.99(m, 2H), 5.55(d, J=10.0Hz, 1H), 5.11(s, 2H), 4.22-4.17( m, 1H), 3.78-3.39(m, 13H), 3.22-3.06(m, 3H), 1.97-1.90(m, 1H), 1.48-1.33(m, 2H), 0.92(d, J=4.00Hz, 3H), 0.89(d, J=4.80Hz, 3H) (S)-4-Hydroxy-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide 1H-NMR (400MHz, CDCl3) δ8.20(s, 1H), 7.65(d, J=8.80Hz, 2H), 6.83(d, J=8.80Hz, 2H), 5.65(d, J=9.60Hz, 1H), 4.31-4.26(m, 1H), 3.84-3.19(m, 16H), 1.99-1.93(m, 1H), 1.53-1.52(m, 2H), 0.93(t, J=6.20Hz, 6H) (S)-Benzyl 4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoate 1 H-NMR (400MHz, CDCl3) δ8.19-8.16(m, 2H), 7.92-7.89(m, 2H), 7.45-7.34(m, 5H), 5.76(d, J=9.20Hz, 1H), 5.37(s, 2H), 4.34-4.28(m, 1H), 3. 82-3.76(m, 1H), 3.68-3.63(m, 1H), 3.58-3.07(m, 14H), 1.97-1.90(m, 1H), 1.50-1.34(m, 2H), 0.94(d, J=6.40Hz, 3H), 0.91(d, J=6.80Hz, 3H) (S)-Tartyl 3-(4-methylphenylsulfonamido)-4-morpholino-4-oxobutanoate 1 H-NMR (400MHz, CDCl3) δ7.72(d, J=8.40Hz, 2H), 7.31(d, J=7.60Hz, 2H), 5.89(d, J= 9.60Hz, 1H), 4.55-4.498(m, 1H), 3.62-3.28(m, 8H), 2.55-2.40(m, 4H), 1.41(m, 9H) (S)-4-Methyl-N-(1-morpholino-1-oxo-3-phenylpropan-2-yl)benzenesulfonamide 1H-NMR (400MHz, CDCl3) δ7.68(d, J=4.80Hz, 2H), 7.23-7.29(m, 5H), 7.11-7.16(m, 2H), 5.88(d, J=9.60Hz, 1H), 4.29-4. 35(m, 1H), 3.22-3.34(m, 3H), 3.05-3.14(m, 2H), 2.90-2.98(m, 2H), 2.74-2.81(m, 1H), 2.55-2.61(m, 2H), 2.40(s, 3H) (S)-N-(3-hydroxy-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.74 (d, J=8.40Hz, 2H), 7.32 (d, J=8.4Hz, 2H), 6.00 (d, J=8.80Hz, 1H) , 4.19-4.24(m, 1H), 3.52-3.68(m, 4H), 3.34-3.49(m, 6H), 2.82(q, J=4.30Hz, 1H), 2.44(s, 3H) (S)-4-Methyl-N-(3-methyl-1-morpholino-1-oxobutan-2-yl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.69(d, J=8.40Hz, 2H), 7.29(d, J=8.40Hz, 2H), 5.66(d, J=9.20Hz, 1H), 3.81(q, J=4.80Hz, 1H), 3.51 -3.58(m, 2H), 3.24-3.35(m, 5H), 3.10-3.17(m, 1H), 2.42(s, 3H), 1.76-1.84(m, 1H), 1.02(d, J=6.80Hz, 3H), 0.88(d, J=6.80 Hz, 3H) (R)-N-(3-mercapto-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1H-NMR(400 MHz, CDCl3)δ7.76(d, J=8.00Hz, 2H), 7.33(d, J=8.00Hz, 2H), 5.95(d, J=9.60Hz, 1H), 4.48-4.53(m, 1H), 3.5 4-3.63(m, 2H), 3.30-3.45(m, 6H), 2.95(dd, J=7.00, 13.8Hz, 1H), 2.84(dd, J=6.20, 14.2Hz, 1H), 2.44(s, 3H) (2S,3S)-3-Hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide 1 H-NMR (400MHz, DMSO-d6) δ8.44(s, 1H), 7.77(d, J=7.20Hz, 2H), 7.28-7.30(m, 3H), 6.82(d, J=8.80Hz, 2H), 5.95(d, J=7.20Hz, 1H) , 4.38-4.40(m, 1H), 3.84(t, J=4.60Hz, 4H), 3.77(dd, J=2.20, 6.60Hz, 1H), 3.08-3.10(m, 5H), 2.39(s, 3H), 0.96(d, J=6.40Hz, 3H) (2S,3S)-3-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.57(s, 1H), 7.84(d, J=7.60Hz, 1H), 7.61(d, J=8.40Hz, 2H), 7.18(d, J=8.0 0Hz, 2H), 7.11(d, J=9.20Hz, 2H), 6.80(d, J=8.80Hz, 2H), 3.71(t, J=4.80Hz, 4H), 3.57(t, J=7.60Hz, 1H), 3.00(t, J=4.60Hz, 4H), 2.20(s, 3H), 1.50-1.63(m, 2H), 1.08-1.12(m, 1H), 0.76-0.79(m, 6H) (S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, DMSO-d6) δ9.63(s, 1H), 8.00(s, 1H) 7.66(d, J=7.60Hz, 2H), 7.23-7.29(m, 4H), 6.84(d, J=8.80Hz) , 2H), 3.87(q, J=6.80Hz, 1H), 3.71(t, J=4.60Hz, 4H), 3.01(t, J=4.40Hz, 4H), 2.29(s, 3H), 1.12(d, J=7.20Hz, 3H) (S)-2-(4-methylphenylsulfonamido)-4-(methylthio)-N-(4-morpholinophenyl)butanamide 1 H-NMR (400MHz, DMSO-d6) δ10.06(s, 1H), 8.42(s, 1H), 8.03(d, J=8.00Hz, 2H), 7.63(d, J=8.40Hz, 2H), 7.59(d, J=9.20Hz, 2H), 7.21(d, J=8.8 0Hz, 2H), 4.26-4.29(m, 1H), 4.09(t, J=4.40Hz, 4H), 3.76(s, 3H), 3.39(t, J=4.60Hz, 4H), 2.74-2.87(m, 2H), 2.33(s, 3H), 2.05-2.25(m, 2H) (S)-3-(1H-indol-2-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.75(s, 1H), 9.64(s, 1H), 8.05(s, 1H), 7.50(d, J=8.00Hz, 2H), 7. 39(d, J=7.60Hz, 1H), 7.27(d, J=8.40Hz, 1H), 7.18(d, J=9.20Hz, 2H), 7.09(d, J=8.40Hz, 2H), 7 .06(d, J=2.00Hz, 1H), 7.02(t, J=7.40Hz, 1H), 6.91(t, J=7.20Hz, 1H), 6.81(d, J=8.80Hz, 2H) , 3.99-4.06(m, 1H), 3.71(t, J=4.80Hz, 4H), 2.99-3.05(m, 5H), 2.79-2.85(m, 1H), 2.18(s, 3H) (S)-3-(1-methyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.04 (s, 1H), 7.48 (d, J=8.20Hz, 2H), 7.17-7.31 (m, 5H ), 7.06(d, J=8.20Hz, 2H), 7.00(dt, J=1.10, 7.20Hz, 1H), 6.82(d, J=9.00Hz, 2H ), 6.76(s, 1H), 5.17(d, J=6.20Hz, 1H), 4.01(q, J=6.20Hz, 1H), 3.82-3.87(m, 3 H), 3.67(s, 2H), 3.17(dd, J=2.93, 6.46Hz, 1H), 3.07-3.12(m, 2H), 2.34(s, 3H) (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide 1 H-NMR (400MHz, DMSO-d6) δ9.64(s, 1H), 8.11(s, 1H), 7.48(d, J=7.60Hz, 2H), 7.12-7.20(m, 9H), 6.81(d, J=8.40Hz, 2H) , 4.03-4.05(m, 1H), 3.71(t, J=4.40Hz, 4H), 3.01(t, J=4.40Hz, 4H), 2.85-2.90(m, 1H), 2.70-2.73(m, 1H), 2.24(s, 3H) (S)-Benzyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate 1 H-NMR (400MHz, CDCl3) δ7.66-7.73(m, 2H), 7.30-7.38(m, 3H), 7.15-7.24(m, 4H), 5.20(d, J=10.1Hz, 1H), 4 .79-4.89(m, 2H), 3.98(ddd, J=6.20, 8.30, 10.0Hz, 1H), 2.39(s, 3H), 1.72-1.85(m, 1H), 1.43-1.55(m, 2H) , 0.87(dd, J=6.60, 7.80Hz, 6H) (S)-Benzyl 4-methyl-2-(4-methylbenzamido)pentanoate 1 H-NMR (400MHz, CDCl3) δ7.69(d, J=8.00 Hz, 2H), 7.39-7.32(m, 5H), 7.24(d, J=8.40Hz, 2H), 6.48(d, J=7.60Hz, 1H), 5.20(d, J=1.20Hz, 2H) , 4.93-4.87(m, 1H), 2.40(s, 3H), 1.80-1.62(m, 3H), 0.97(d, J=6.00Hz, 3H), 0.95(d, J=6.00Hz, 3H) (S)-Benzyl 2-(4-tert-butylbenzamido)-4-methylpentanoate 1 H-NMR (400MHz, CDCl3) δ7.74-7.72(m, 2H), 7.52-7.44(m, 2H), 7.37-7.31(m, 5H), 6.49(d, J=8.40Hz, 1H), 5. 19(s, 2H), 4.94-4.88(m, 1H), 1.78-1.63(m, 3H), 1.33(s, 9H), 0.97(d, J=6.00Hz, 3H), 0.94(d, J=5.60Hz, 3H) (S)-Benzyl 2-(benzo[d][1,3]dioxole-5-carboxamido)-4-methylpentanoate 1 H-NMR (400MHz, CDCl3) δ7.71(dd, J=2.00, 8.00Hz, 1H), 7.51(d, J=2.00Hz, 1H), 7.38-7.33(m, 5H), 6.86(d, J=8.40Hz, 1H), 6.06(s, 2H), 5.16( d, J=1.20Hz, 2H), 3.56-3.52(m, 1H), 1.78-1.73(m, 1H), 1.63-1.56(m, 1H), 1.48-1.41(m, 1H), 0.93(d, J=6.40Hz, 3H), 0.91(d, J=6.80Hz, 3H) (S)-Benzyl 2-(4-(tert-butoxycarbonylamino)benzamido)-4-methylpentanoate 1H-NMR (400MHz, CDCl3) δ7.75-7.72(m, 2H), 7.43(d, J=8.40Hz, 2H), 7.39-7.31(m, 5H), 6.61(s, 1H), 6.43(d, J=8.40H) z, 1H), 5.19(d, J=2.00Hz, 2H), 4.92-4.86(m, 1H), 1.78-1.62(m, 3H), 0.97(d, J=6.00Hz, 3H), 0.95(d, J=6.40Hz, 3H) (S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate 1 H-NMR (400MHz, CDCl3) δ7.91-7.89(m, 2H), 7.68-7.54(m, 3H), 7.38-7.31(m, 5H), 5.97(d, J=8.00Hz, 1H), 5.1 4(s, 2H), 4.61-4.56(m, 1H), 3.46-3.40(m, 2H), 2.71-2.66(m, 2H), 1.64-1.50(m, 3H), 0.90(d, J=5.60Hz, 6H) (S)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.54 (brs, 1H), 7.75 (t, J=7.60Hz, 4H), 7.26 (d, J=8 .20Hz, 2H), 6.99(d, J=0.70Hz, 1H), 6.95(d, J=8.20Hz, 2H), 5.19(d, J=7.00H) z, 1H), 3.91(d, J=5.00Hz, 1H), 3.84(d, J=0.70Hz, 3H), 2.32(s, 3H), 1.53-1. 63(m, 2H), 1.43-1.51(m, 1H), 0.84(d, J=5.80Hz, 3H), 0.68(d, J=5.80Hz, 3H) (S)-1-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-phenylurea 1H-NMR (400MHz, CDCl3) δ7.80(s, 1H), 7.26-7.17(m, 4H), 6.94-6.90(m, 1H), 6.72(d, J=8.80Hz, 1H), 5.03-4.97( m, 1H), 3.81-3.57(m, 8H), 1.84-1.77(m, 1H), 1.61-1.43(m, 2H), 0.90(d, J=3.60Hz, 3H), 0.87(d, J=7.20Hz, 3H) (S)-4-tert-butyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzamide 1 H-NMR (400MHz, DMSO-d6) δ8.40(s, 1H), 7.81(d, J=8.00Hz, 2H), 7.45(d, J=8.80Hz, 2H), 4. 82-4.73(m, 1H), 3.53-3.42(m, 8H), 1.74-1.50(m, 3H), 1.28(s, 9H), 0.89(d, J=6.80Hz, 6H) (S)-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-(phenylsulfonyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ8.30(d, J=8.80Hz, 1H), 7.88-7.86(m, 2H), 7.75(t, J=8.00Hz, 1H), 7.65(d, J=8.00Hz, 2H), 4 .66-4.61(m, 1H), 3.52-3.25(m, 10H), 2.46-2.42(m, 2H), 1.52-1.46(m, 1H), 1.38-1.33(m, 2H), 0.82(d, J=6.60Hz, 6H) (S)-4-tert-butyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide 1H-NMR (400MHz, MeOD) δ7.81(d, J=8.00Hz, 2H), 7.51(t, J=8.80Hz, 2H), 7.45(d, J=8.80Hz, 2H), 6.94(d, J=8.80Hz, 2H), 4 .85-4.81(m, 1H), 3.82(t, J=5.00Hz, 3H), 3.10(t, J=4.80Hz, 3H), 1.82-1.62(m, 3H), 1.28(s, 9H), 1.03(d, J=6.60Hz, 6H) (S)-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzo[d][1,3]dioxole-5-carboxamide 1 H-NMR (400MHz, DMSO-d6) δ9.84(s, 1H), 8.35(d, J=7.60Hz, 1H), 7.52-7.44(m, 4H), 6.97(d, J=8.40Hz, 1H), 6.87(d, J=9.20Hz, 2H), 6.08(d, J=2. 40Hz, 2H), 4.60-4.54(m, 1H), 3.71(d, J=4.80Hz, 4H), 3.02(t, J=4.80Hz, 4H), 1.74-1.50(m, 3H), 0.92(d, J=6.80Hz, 3H), 0.89(d, J=6.40Hz, 3H) (S)-4-Methyl-N-(4-morpholinophenyl)-2-(3-(phenylsulfonyl)propanamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.69-8.63(m, 1H), 7.87(d, J=7.20Hz, 2H), 7.71-7.32(m, 5H), 7.18-6.60(m, 3H), 4.59-4.55(m, 1H), 3 .82(t, J=5.00Hz, 3H), 3.54-3.48(m, 2H), 3.06(t, J=4.80Hz, 3H), 2.75-2.73(m, 2H), 1.85-1.56(m, 3H), 0.89(d, J=6.2Hz, 6H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.44(s, 1H), 10.78(s, 1H), 8.51(brs, 1H), 7.82-7.80(d, J=8.50Hz, 2H), 7.47-7.37(m, 6H), 7.28-7.26(d, J=8.0 0Hz), 7.08-6.90(m, 5H), 4.32(brs, 1H), 3.79(s, 3H), 3.33(s, 2H), 3.11-3.07(dd, J=14.5, 6.00Hz, 1H), 2.90-2.85(dd, J=14.0, 8.50Hz, 1H) (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.3(s, 1H), 10.7(s, 1H), 8.24-8.22(d, J=8.50Hz, 1H), 7. 95-7.93(d, J=8.50Hz, 1H), 7.50-7.48(d, J=8.50Hz, 2H), 7.15-7.09(m, 4H), 6.97-6. 95(d, J=8.00Hz, 1H), 6.74-6.58(m, 6H), 4.01-3.96(q, J=7.50Hz, 1H), 3.47(s, 3H), 2 .79-2.74(dd, J=14.2, 7.00Hz, 1H), 2.56-2.51(dd, J=14.5, 8.00Hz, 1H), 1.86(s, 3H) (S)-3-(1H-indol-3-yl)-2-(2-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, CDCl3) δ8.27(s, 1H), 7.86-7.83(m, 2H), 7.33-7.29(m, 3H), 7.20-7.14(m, 4H), 7.01-6.95(m, 2H), 6.91(d, J=2.40Hz, 4H), 6 .80-6.78(m, 2H), 5.38(d, J=5.60Hz, 1H), 4.00-3.95(m, 1H), 3.83(t, J=4.60Hz, 4H), 3.27-3.14(m, 2H), 3.07(t, J=5.00Hz, 4H), 2.23(s, 3H) (S)-3-(1H-indol-3-yl)-2-(3-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.76(s, 1H), 9.70(s, 1H), 8.11(s, 1H), 7.45-7.39(m, 3H), 7.28-7.19(m, 5H), 7.06-7.00(m, 2H), 6.93- 6.89(m, 1H), 6.81(d, J=8.80Hz, 2H), 4.09-4.07(m, 1H), 3.71(t, J=4.80Hz, 4H), 3.05-2.99(m, 5H), 2.85-2.79(m, 1H), 2.14(s, 3H) (S)-2-(3,5-dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.77(s, 1H), 9.71(s, 1H), 8.04(s, 1H), 7.42(d, J=8.00Hz, 1H), 7.28-7.22(m, 5H), 7.07-7.00(m, 3H), 6.92( t, J=7.40Hz, 1H), 6.82(d, J=9.20Hz, 2H), 4.11-4.07(m, 1H), 3.71(t, J=4.80Hz, 4H), 3.05-2.99(m, 5H), 2.85-2.80(m, 1H), 2.12(s, 6H) (S)-2-(4-fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.77(d, J=2.00Hz, 1H), 9.75(s, 1H), 8.26(s, 1H), 7.62-7.59(m, 2H), 7.46(d, J=8.00Hz, 1H), 7.28-7.22(m, 3H) ), 7.09-7.01(m, 4H), 6.93(t, J=7.40Hz, 1H), 6.85-6.81(m, 2H), 4.10(s, 1H), 3.72(t, J=4.80Hz, 4H), 3.07-3.01(m, 5H), 2.89-2.83(m, 1H) (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfonamido)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.77(d, J=1.60Hz, 1H), 9.79(s, 1H), 8.55(s, 1H), 7.72(d, J=8. 80Hz, 2H), 7.57(d, J=8.40Hz, 2H), 4.47(d, J=8.00Hz, 1H), 7.25(d, J=7.60Hz, 1H), 7.19(d, J =9.20Hz, 2H), 7.11(d, J=2.40Hz, 1H), 7.02(t, J=7.60Hz, 1H), 6.92(t, J=7.40Hz, 1H), 6.81( d, J=9.20Hz, 2H), 4.14(s, 1H), 3.72(t, J=4.60Hz, 4H), 3.08-2.99(m, 5H), 2.92-2.86(m, 1H) (S)-3-(5-hydroxy-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, DMSO-d6) δ10.45(d, J=2.00Hz, 1H), 9.63(s, 1H), 8.54(s, 1H), 8.02(s, 1H), 7.53(d, J= 8.00Hz, 2H), 7.18(d, J=9.20Hz, 2H), 7.11(d, J=8.20Hz, 2H), 7.07(d, J=8.40Hz, 1H), 6.97(d, J=2.40H) z, 1H), 6.81(d, J=8.00Hz, 2H), 6.77(d, J=2.00Hz, 1H), 6.57(dd, J=2.00, 8.40Hz, 1H), 4.09-4.06(s, 1 H), 3.72(t, J=4.80Hz, 4H), 3.01(t, J=5.00Hz, 4H), 2.96-2.91(m, 1H), 2.76-2.70(m, 1H), 2.23(s, 3H) (S)-N-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ8.19 (brs, 1H), 7.67-7.71 (m, 2H), 7.48 (d, J=7.83Hz, 1H), 7.34 (d, J=8.22 Hz, 1H), 7.25(d, J=7.83Hz, 2H), 7.18(dt, J=1.17, 7.63Hz, 1H), 7.07-7.12(m, 1H), 7.06(d, J=1.96 Hz, 1H), 5.92(d, J=9.78Hz, 1H), 4.42(dt, J=5.28, 9.88Hz, 1H), 3.19-3.34(m, 4H), 3.08-3.15(m, 1H) ), 2.86-2.98(m, 2H), 2.75(m, 1H), 2.62-2.70(m, 1H), 2.50-2.56(m, 1H), 2.39(s, 3H), 2.19(m, 1H).

[0051] (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)propanamide 1H-NMR (400MHz, CDCl3) δ8.20-8.24(m, 1H), 7.54(d, J=8.22Hz, 2H), 7.20(d, J=8.22Hz, 2H), 7.01-7.10(m, 3H), 6.91(t, J=7.43Hz, 1H), 6.86(d, J=2) .35Hz, 1H), 6.48(s, 1H), 6.17-6.23(m, 1H), 4.27(d, J=6.65Hz, 1H), 3.78 (t, J=4.70Hz, 4H), 3.16(d, J=6.65Hz, 2H), 2.87-2.99(m, 4H), 2.25(s, 3H) (S)-2-(2,4-dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.75(s, 1H), 9.58(s, 1H), 7.98(s, 1H), 7.54(d, J=8.00H z, 1H), 7.38 (d, J=8.00Hz, 1H), 7.28 (d, J=8.40Hz, 1H), 7.19 (d, J=9.20Hz, 2H), 7.08 (d, J=2.40Hz, 1H), 7.02(t, J=7.40Hz, 1H), 6.90-6.81(m, 5H), 4.05-4.03(m, 1H), 3. 72(t, J=4.60Hz, 4H), 3.04-3.00(m, 5H), 2.90-2.85(m, 1H), 2.39(s, 3H), 2.15(s, 3H) 3-(3-ethoxy-2-(4-methylphenylsulfonamido)-3-oxopropyl)-1H-indole e-5-carboxylic acid 1 H-NMR (400MHz, CDCl3) δ12.37(s, 1H), 11.17(s, 1H), 8.37(d, J=8.40Hz, 1H), 8.01(s, 1H), 7.68(dd, J=1.40, 8.60Hz, 1H), 7.48(d, J=8.00Hz, 1H), 7.35(d, J=8.40Hz, 1H), 7.20-7.08(m, 3H), 3.96-3.90(m, 1H), 3.0 8-3.06(m, 1H), 2.94-2.88(m, 1H), 2.31(s, 1H), 0.86(t, J=6.60Hz, 3H) (S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(1-tosyl-1H-imidazol-4-yl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.62(s, 1H), 7.84(s, 1H), 7.71(t, J=8.40Hz, 4H), 7. 29-7.23(m, 6H), 6.98(s, 1H), 6.89(d, J=6.40Hz, 1H), 6.83(dt, J=8.80Hz, 2H ), 3.99-3.97(m, 1H), 3.85(t, J=4.80Hz, 4H), 3.10(t, J=4.80Hz, 4H), 3.01(d d, J=5.60, 15.2Hz, 1H), 2.61(dd, J=4.80, 14.8Hz, 1H), 2.40(d, J=8.40Hz, 6H) (S)-N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (400MHz, CDCl3) δ8.14 (brs, 1H), 8.00 (d, J=2.35Hz, 1H), 7.86 (s, 1H), 7.62 (dd, J=2.74, 9.00Hz, 1H), 7 .49-7.53(m, 2H), 7.33(dd, J=3.91, 7.83Hz, 2H), 7.20(t, J=7.63Hz, 1H), 7.08-7.12(m, 2H), 7.02(t, J=7.63Hz) , 1H), 6.96(d, J=1.96Hz, 1H), 6.57(d, J=9.00Hz, 1H), 5.11(d, J=6.26Hz, 1H), 4.05(q, J=6.52Hz, 1H), 3.97(d, J=11.35Hz, 2H), 3.67-3.77(m, 2H), 3.12-3.28(m, 2H), 2.45-2.53(m, 2H), 2.36(s, 3H), 1.27(d, J=6.26Hz, 6H) (R)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, CDCl3) δ8.80 (brs, 1H), 8.27 (s, 1H), 7.97 (s, 2H), 7.45-7.48 (m, 2H), 7.32(d, J=7.83Hz, 1H), 7.29(d, J=3.52Hz, 1H), 7.22(s, 1H), 7.13(t, J=7.43 Hz, 1H), 7.00(d, J=8.22Hz, 2H), 6.94(s, 1H), 6.78-6.81(m, J=9.00Hz, 2H), 5.57(d, J=6.65Hz, 1H), 4.0 5(d, J=6.65Hz, 1H), 3.80-3.86(m, 4H), 3.19(dd, J=6.46, 13.50Hz, 2H), 3.05-3.10(m, 4H), 2.28(s, 3H) (S)-N-(3-fluoro-4-morpholinophenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.78(s, 1H), 9.90(s, 1H), 8.16(brs, 1H), 7.51(d, J=8.22Hz, 2H ), 7.40(d, J=7.83Hz, 1H), 7.29(d, J=7.83Hz, 1H), 7.22(dd, J=2.15, 15.1Hz, 1H), 7.09(d, J= 8.61Hz, 3H), 7.04(t, J=7.63Hz, 1H), 6.89-6.99(m, 3H), 4.06(brs, 1H), 3.70-3.74(m, 4H), 3 .04(dd, J=6.85, 14.3Hz, 1H), 2.90-2.94(m, 4H), 2.85(dd, J=7.40, 14.4Hz, 1H), 2.21(s, 3H) (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)propanamide 1H-NMR (400MHz, DMSO-d6) δ10.71(brs, 1H), 9.90(s, 1H), 8.66(brs, 1H), 7.84-7.90(m, 2H), 7.56-7.61(m, 2H), 7.48(d, J=7.83Hz, 1H), 7.29-7.35(m, J=9.00Hz, 2H), 7.12(d, J=7.83Hz, 1H), 7.05-7.08(m, 1H), 6.87-6.96(m, 2H), 6.81-6.86(m, 2H), 4.13(dd, J=5 .28, 9.19Hz, 1H), 3.70-3.75(m, 4H), 2.98-3.05(m, 5H), 2.88(dd, J=9.78, 14.5Hz, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.77(brs, 1H), 9.77(s, 1H), 8.35(brs, 1H), 7.40 -7.48(m, 5H), 7.28(d, J=8.22Hz, 1H), 7.19-7.24(m, 2H), 7.07-7.11(m, 1H), 7 .04(t, J=7.43Hz, 1H), 6.91-6.96(m, 1H), 6.81-6.86(m, 2H), 4.10(t, J=7.24 Hz, 1H), 3.69-3.75(m, 4H), 3.00-3.08(m, 5H), 2.86(dd, J=8.41, 14.28Hz, 1H) (S)-3-(1H-indol-3-yl)-2-(4-methoxyphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, DMSO-d6) δ10.78(brs, 1H), 9.67(s, 1H), 7.99(brs, 1H), 7.54(d, J=8 .61Hz, 2H), 7.41(d, J=7.83Hz, 1H), 7.28(d, J=8.22Hz, 1H), 7.22(d, J=9.00Hz, 2H), 7 .07-7.10(m, 1H), 7.03(t, J=7.63Hz, 1H), 6.90-6.95(m, 1H), 6.81(t, J=9.59Hz, 4H), 4.06(brs, 1H), 3.70-3.74(m, 4H), 3.69(s, 3H), 2.98-3.07(m, 5H), 2.80-2.90(m, 1H) (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4 morpholinophenyl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.09(brs, 1H), 8.03(s, 1H), 7.81(s, 1H), 7.58-7.62(m, 2H), 7. 33-7.38(m, 2H), 7.18-7.25(m, 5H), 7.05(t, J=7.43Hz, 1H), 6.97(d, J=2.35Hz, 1H), 6.8 0-6.85(m, J=9.00Hz, 2H), 5.11(d, J=6.26Hz, 1H), 4.08(d, J=6.26Hz, 1H), 3.83-3.89(m , 4H), 3.34(dd, J=6.06, 14.28Hz, 1H), 3.09-3.16(m, 5H), 1.25(dd, J=2.35, 7.04Hz, 6H) (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (400MHz, CDCl3) δ7.74(d, J=8.40Hz, 2H), 7.67(d, J=7.60Hz, 2H), 7.21(t, J=6.80Hz, 4H), 7.04(s, 1H), 3 .98-3.95(m, 1H), 2.37(s, 1H), 2.26(m, 3H), 1.64-1.49(m, 3H), 0.85(d, J=6.40Hz, 3H), 0.72(d, J=6.40Hz, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.13(s, 1H), 10.83(s, 1H), 8.26-8.24(d, J=8.50Hz, 1H), 7 .45-7.44(d, J=8.00Hz, 2H), 7.39-7.38(d, J=7.50Hz, 1H), 7.29-7.27(d, J=8.00Hz, 1H ), 7.06-7.02(m, 4H), 6.91-6.89(m, 1H), 6.72(s, 1H), 4.27-4.22(m, 1H), 3.07-3.03(d d, J=14.2, 7.50Hz, 1H), 2.86-2.81(dd, J=14.2, 8.00Hz, 1H), 2.24(s, 3H), 2.22(s, 3H) (S)-N-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.4(s, 1H), 10.8(s, 1H), 8.32(m, 1H), 7.91(m, 1H), 7.72(m, 1H), 7.47-7.44(m, 6H), 7.03-6.91(m, 5H), 4.34(brs, 1H), 3.11(m, 1H), 2.91(m, 1H), 2.08(s, 3H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanoic acid 1H-NMR (500MHz, DMSO-d6) δ12.73 (brs, 1H), 10.80 (s, 1H), 8.41-8.39 (d, J=8.50 Hz, 1H), 7.51-7.49(d, J=8.50Hz, 2H), 7.42-7.40(d, J=8.00Hz, 2H), 7.32-7.29( t, J=8.00Hz, 2H), 7.08-7.03(m, 2H), 6.94-6.91(t, J=7.50Hz, 1H), 3.94-3.89( m, 1H), 3.10-3.08(dd, J=14.5, 6.00Hz, 1H), 2.89-2.84(dd, J=14.0, 8.50Hz, 1H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.71(d, J=8.00Hz, 2H), 7.16(d, J=8.00Hz, 2H), 6.95(s, 1H), 6.35(d, J=10.0Hz, 1H), 4.14-4.06(m, 1H), 3.8 6(t, J=4.80Hz, 4H), 3.13-3.07(m, 4H), 2.29(s, 3H), 1.75-1.70(m, 1H), 1.60-1.53(m, 1H), 1.46-1.41(m, 1H), 0.81(d, J=6.80Hz, 6H) (S)-N-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ13.52(s, 1H), 8.14(d, J=8.80Hz, 1H), 7.92-7.88(m, 2H), 7.68(d, J=8.40Hz, 2H), 7.18(d, J=8.40Hz, 2H), 7.07-7.04(m, 2H), 4.36-4.29(m, 1H), 3.91(s, 3H), 2.21(s, 3H), 1.84-1.79(m, 1H), 1.72-1.6 4(m, 1H), 1.59-1.54(m, 1H), 0.89(d, J=6.40Hz, 3H), 0.86(d, J=6.80Hz, 1H) (S)-N-(5-(4-methoxyphenyl)isoxazol-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ10.55(s, 1H), 7.80-7.76(m, 4H), 7.19-7.15(m, 3H), 6.99(d, J=9.20Hz, 2H), 6.43(d, J=9.20Hz, 1H), 4.2 2-4.16(m, 1H), 3.86(s, 3H), 2.21(s, 3H), 1.88-1.83(m, 1H), 1.72-1.59(m, 2H), 0.91(d, J=6.80Hz, 3H), 0.88(d, J=6.40Hz, 3H).

[0052] (S)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.22(s, 1H), 7.78(d, J=8.40Hz, 2H), 7.74-7.71(m, 2H), 7.30(d, J=8.00Hz, 2H), 6.98-6.94(m, 2H), 6.56(s, 1H) , 5.40(d, J=7.20Hz, 1H), 3.97-3.92(m, 1H), 3.85(s, 3H), 2.35(s, 3H), 1.64-1.47(m, 3H), 0.83(d, J=6.40Hz, 3H), 0.66(d, J=5.60Hz, 1H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)pentanamide 1H-NMR (400MHz, CDCl3) δ9.69(s, 1H), 7.91(d, J=8.40Hz, 2H), 7.79(d, J=8.40Hz, 2H), 7.65(d, J=8.40Hz, 2H), 7.29-7.26(m, 2H), 7.2 3(s, 1H), 5.26(d, J=6.80Hz, 1H), 3.97-3.92(m, 1H), 2.33(s, 3H), 1.67-1.45(m, 3H), 0.83(d, J=6.40Hz, 3H), 0.65(d, J=6.40Hz, 3H) (S)-N-(4-(3,4-dimethoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.74(s, 1H), 7.76(d, J=7.60Hz, 2H), 7.38-7.34(m, 2H), 7.26(d, J=6.80Hz, 2H), 7.01(s, 1H), 6.90(d, J=8.00Hz, 1H), 5.4 0(d, J=6.80Hz, 1H), 4.19-4.10(m, 1H), 3.95(s, 3H), 3.90(s, 3H), 2.32( s, 3H), 1.60-1.42(m, 3H), 0.80(d, J=6.00Hz, 3H), 0.63(d, J=5.60Hz, 3H) (S)-N-(4-(2-bromo-4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.62(s, 1H), 7.78-7.75(m, 4H), 7.26(s, 1H), 7.10-7.05(m, 3H), 5.31(d, J=7.60H z, 1H), 3.95-3.92(m, 1H), 2.32(s, 3H), 1.64-1.46(m, 3H), 0.82(d, J=6.40Hz, 3H), 0.66(d, J=6.00Hz, 3H) (S)-4-(2-aminothiazol-4-yl)phenyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate 1H-NMR (400MHz, CDCl3) δ7.79(d, J=7.60Hz, 2H), 7.67(d, J=7.60Hz, 2H), 7.29(d, J=7.20Hz, 2H), 6.68(d, J=7.60Hz, 2H), 6.65(s, 1H), 5. 53(d. (S)-N-(4-(4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.58(s, 1H), 7.79-7.76(m, 3H), 7.28-7.26(m, 2H), 7.11-7.06(m, 2H), 5.20(d, J=6.80Hz, 2 H), 5.27(s, 2H), 3.93-3.91(m, 1H), 2.41(m, 3H), 1.66-1.46(m, 3H), 0.83(d, J=6.40Hz, 3H), 0.65(d, J=6.40Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethoxy)phenyl)thiazol-2-yl)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.60(s, 1H), 7.83(d, J=8.80Hz, 2H), 7.79(d, J=8.00Hz, 2H), 7.29-7.23(m, 4H), 7.13(s, 1H) , 5.21(d, J=6.80Hz, 1H), 3.93(s, 1H), 2.33(m, 3H), 1.65-1.48(m, 3H), 0.83(d, J=6.40Hz, 3H), 0.64(d, J=6.00Hz, 3H) (S)-N-(4-(4-hydroxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1H-NMR (400MHz, CDCl3) δ7.72(d, J=8.00Hz, 2H), 7.64(d, J=8.80Hz, 2H), 7.20(d, J=8.00Hz, 2H), 6.93(s, 1H), 6.88( d, J=8.40Hz, 2H), 3.97-3.93(m, 1H), 2.25(s, 3H), 1.65-1.51(m, 3H), 0.88(d, J=6.40Hz, 3H), 0.75(d, J=6.00Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-p-tolylthiazol-2-yl)pentanamide 1 H-NMR (400 MHz, CDCl 3) )δ7.74(d, J=8.40Hz, 2H), 7.67(d, J=7.60Hz, 2H), 7.21(t, J=6.80Hz, 4H), 7.04(s, 1H), 3.98-3.95( m, 1H), 2.37(s, 1H), 2.26(m, 3H), 1.64-1.49(m, 3H), 0.85(d, J=6.40Hz, 3H), 0.72(d, J=6.40Hz, 3H) (S)-N-(4-(4-((S)-1-methoxypropan-2-yloxy)phenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ9.97(s, 1H), 7.74(d, J=8.40Hz, 2H), 7.69(d, J=8.80Hz, 2H), 7.23(d, J=8.00Hz, 2H), 6.97(s, 1H), 6.95(d, J=9.20Hz, 2H), 5.71(d, J=7.60Hz, 1H), 4 .58-4.54(m, 1H), 4.00-3.94(m, 1H), 3.60-3.46(m, 2H), 3.40(s, 3H), 2.28(s, 3H), 1.5 6-1.40(m, 3H), 1.31(d, J=6.00Hz, 3H), 0.78(d, J=6.00Hz, 3H), 0.66(d, J=5.60Hz, 3H) (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)pentanamide 1 H-NMR (400MHz, CDCl3) δ8.28(dd, J=9.00, 11.4Hz, 4H), 7.19(d, J=8.40Hz, 2H), 6.95(t, J=4.60Hz, 3H), 4.13-3.95(m, 1H), 3.89(t, J=4 .80Hz, 3H), 3.21(t, J=5.00Hz, 3H), 2.25(s, 3H), 1.67-1.64(m, 1H), 1.55-1.51(m, 2H), 0.88(d, J=6.80Hz, 3H), 0.75(d, J=6.40Hz, 3H) (S)-Methyl 4-(2-(4-methyl-2-(4-methylphenylsulfonamido)pentanoyl)thiazol-4-yl)benzoate 1 H-NMR (400MHz, CDCl3) δ10.05(s, 1H), 8.18(d, J=8.00Hz, 2H), 7.93(d, J=8.40Hz, 2H), 7.76(d, J=8.00Hz, 2H), 7.26(s, 1H), 7.20(d, J=8.00Hz) , 2H), 5.63(d, J=8.00Hz, 1H), 4.12-4.09(m, 1H), 3.99(s, 3H), 2.24(s, 3H), 1.65-1.52(m, 1H), 0.86(d, J=5.60Hz, 3H), 0.74(d, J=5.60Hz, 3H) (S)-4-(2-(4-methylphenylsulfonamido)-3-(4-morpholinophenylamino)-3-oxopropyl)phenyl 4-methylbenzenesulfonate 1H-NMR (400MHz, DMSO-d6) δ9.62(s, 1H), 9.18(s, 1H), 8.05(s, 1H), 7.49(d, J=8.00Hz, 2H), 7.15(d, J=8.40Hz, 4H), 6.93(d, J=8.40Hz, 2H), 6 .83(d, J=9.20Hz, 2H), 6.58(d, J=8.00Hz, 2H), 3.95(m, 1H), 3.72(t, J=4.60Hz, 4H), 3.02(t, J=4.60Hz, 4H), 2.78-2.58(m, 2H), 2.25(s, 3H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-imidazol-4-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d67.80-7.71(d, J=9.00Hz, 2H), 7.59(s, 4H), 7.45-7.41(d, J=15.0Hz2H), 6.98-6.96(d, J=11.5Hz, 2H), 6.7 5(brs, 1H), 4.31-4.28(t, J=7.50Hz, 1H), 3.77(s, 3H), 2.92-2.90(dd, J1=14.0, 7.00Hz, 1H), 2.77-2.73(dd, J=14.0, 7.50Hz, 1H) (S)-N-Methoxy-N,4-dimethyl-2-(4-methylphenylsulfonamido)pentanamide 1 H-NMR (400MHz, CDCl3) δ7.72(d, J=8.00Hz, 2H), 7.27(d, J=8.40Hz, 2H), 5.40(d, J=10.4Hz, 1H), 4.28(t, J=10.4Hz, 1H), 3.56(s, 3H), 2.92(s, 3H), 2.40(m, 3H), 1.92-1.89(m, 1H), 1.45-1.39(m, 3H), 1.31-1.24(m, 1H), 0.91(d, J=6.40Hz, 6H) (S)-3-(1H-indol-3-yl)-N-methoxy-N-methyl-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (400MHz, CDCl3) δ8.00(s, 1H), 7.54(d, J=8.40Hz, 2H), 7.44(d, J=7.60Hz, 1H), 7.31(d, J=8.00Hz, 1H), 7.16(t, J=7.40Hz, 1H), 7. 11-7.03(m, 4H), 5.46(d, J=9.60Hz, 1H), 4.61-4.55(m, 1H), 3.45(s, 3H), 3.17-3.12(m, 1H), 3.05-3.00(m, 1H), 2.95(s, 3H), 2.34(m, 3H) (S)-N-(3-(1H-indol-3-yl)-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)propan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ8.25(s, 1H), 7.60(d, J=8.40Hz, 2H), 7.47(d, J=8.00Hz, 1H), 7.29-7.26(m, 1H), 7.14-7 .02(m, 5H), 5.86(d, J=9.60Hz, 1H), 4.66-4.60(m, 1H), 3.67-3.63(m, 1H), 3.58-3.36(m, 13H), 3.25-2.97(m, 4H) (S)-2-(4-tert-butylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, CD3OD) δ7.94(s, 1H), 7.58-7.62(m, 2H), 7.39(d, J=7.83Hz, 1H), 7.30-7.34(m, 2H), 7.25(d, J=7.83Hz, 1H), 6.99-7 .04(m, 4H), 6.90(s, 1H), 6.77(d, J=9.00Hz, 2H), 4.06(s, 1H), 3.75-3.79(m, 4H), 3.12-3.20(m, 1H), 2.98-3.05(m, 5H), 1.18(s, 9H) (S)-2-(4-bromophenylsulfonamido)-N-(4-(2-chlorophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.89-2.93(dd, J=14.67, 8.80Hz, 1H), 3.10-3.14(dd, J=14.18, 6.35 Hz, 1H), 4.34(brs, 1H), 6.91-6.94(t, J=7.33Hz, 1H), 7.04-7.07(t, J=7.82Hz, 1H), 7.11(s, 1H) , 7.28-7.30(d, J=8.31Hz, 1H), 7.37-7.45(m, 6H), 7.47-7.49(d, J=7.82Hz, 1H), 7.55-7.57(d, J=7.82Hz, 1H), 7.60(s, 1H), 7.81-7.83(m, 1H), 8.55(brs, 1H), 10.80(brs, 1H), 12.53(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-N-(4-(2,4-dimethoxyphenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.85-2.90 (dd, J=14.18, 8.80Hz, 1H), 3.08-3.12 (dd, J=14.67, 6.35Hz, 1H), 3.80 (s, 3H), 3.90(s, 3H), 4.32-4.34(d, J=6.35Hz, 1H), 6.61-6.63(d, J=8.80Hz, 1H), 6.66(s, 1H), 6.90-6.93(t , J=7.33Hz, 1H), 7.03-7.06(t, J=7.33Hz, 1H), 7.08(s, 1H), 7.26-7.28(d, J=7.82Hz, 1H), 7.36-7.40(m, 4H) , 7.47-7.48(m, 2H), 7.96-7.98(d, J=8.80Hz, 1H), 8.51-8.52(d, J=6.84Hz, 1H), 10.78(s, 1H), 12.39(s, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.34(s, 1H), 10.80(s, 1H), 8.53(s, 1H), 7.48-7.45(m, 2H), 7.40-7.36(m, 4H), 7.30-7.27 (m, 1H), 7.23-7.20(m, 1H), 7.10-7.02(m, 2H), 6.95-6.90(m, 1H), 4.33(brs, 1H), 3.12-3.07(m, 1H), 2.92-2.86(m, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(5-methylthiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.10(s, 1H), 10.80(s, 1H), 8.50-8.45(d, J=8.00Hz, 1H), 7.46-7.45(d, J=7.50Hz, 1H), 7.41-7.36(m, 4H), 7.29-7.27(d, J=8.00Hz, 1 H), 7.11-7.03(m, 3H), 6.93-6.90(t, J=7.00Hz, 1H), 4.32-4.27(m, 1H), 3.08-3. 04(dd, J=14.20, 6.50Hz, 1H), 2.89-2.85(dd, J=14.20, 8.50Hz, 1H), 2.52(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide 1H-NMR (500MHz, DMSO-d6) δ12.2(s, 1H), 10.8(s, 1H), 8.53-8.52(d, J=8.50Hz, 1H ), 7.45-7.44(d, J=8.00Hz, 1H), 7.39(m, 4H), 7.28-7.27(d, J=8.00Hz, 1H), 7.07- 7.02(m, 2H), 6.92-6.90(t, J=7.00Hz, 1H), 6.75(s, 1H), 4.29-4.25(m, 1H), 3.09 -3.05(dd, J=14.2, 6.00Hz, 1H), 2.89-2.85(dd, J=14.7, 8.00Hz, 1H), 2.52(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-methylthiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.01(s, 1H), 10.79(s, 1H), 8.25(d, J=8.00Hz, 1H) , 7.46-7.44(m, 2H), 7.40-7.39(d, J=7.50Hz, 1H), 7.29-7.27(d, J=8.00Hz, 1H) , 7.10-7.02(m, 5H), 6.93-6.90(m, 1H), 4.28-4.26(m, 1H), 3.04-3.03(dd, J=14 .2, 7.00Hz, 1H), 2.86-2.84(dd, J=14.2, 7.00Hz, 1H), 2.32(s, 3H), 2.22(s, 3H) (S)-Methyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate 1H-NMR(400 MHz, DMSO-d6)δ10.74(s, 1H), 9.77(s, 1H), 8.44(s, 1H), 7.74(d, J=8.40Hz, 2H), 7 .62(d, J=8.00Hz, 2H), 7.44(d, J=7.20Hz, 1H), 7.22(t, J=8.40Hz, 3H), 7.08(d, J=2 .00Hz, 1H), 6.99(d, J=7.40Hz, 1H), 6.90(t, J=7.20Hz, 1H), 6.81(d, J=9.20Hz, 2H ), 4.13-4.09(m, 1H), 3.72(t, J=4.60Hz, 4H), 3.05-3.00(m, 5H), 2.89-2.83(m, 1H) (S)-Ethyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate 1 H-NMR (400MHz, DMSO-d6) δ10.74(s, 1H), 9.76(s, 1H), 7.73(d, J=8.80Hz, 2H), 7.62(d , J=8.40Hz, 2H), 7.44(d, J=7.60Hz, 1H), 7.23-7.20(m, 3H), 7.09(d, J=2.40Hz, 1H), 7 .00-6.81(m, 2H), 6.81(d, J=9.20Hz, 2H), 4.31(d, J=7.10Hz, 2H), 4.12-4.09(m, 1H), 3.72(t, J=4.60Hz, 4H), 3.05-3.00(m, 5H), 2.89-2.83(m, 1H), 1.34(t, J=7.00Hz, 3H) (S)-3-(4-benzoylphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, DMSO-d6) δ9.75(s, 1H), 7.68(d, J=7.20Hz, 3H), 7.57(t, J=5 .80Hz, 4H), 7.47(d, J=8.00Hz, 2H), 7.33(d, J=8.00Hz, 2H), 7.20(d, J=8.80H z, 2H), 7.12 (d, J=7.60Hz, 2H), 6.85 (d, J=8.80Hz, 2H), 4.31 (d, J=7.10Hz, 2H) ), 4.12-4.09(m, 1H), 3.72(t, J=4.40Hz, 4H), 3.04-2.95(m, 5H), 2.20(s, 3H) (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)-N-methylbenzamide 1 H-NMR (400MHz, DMSO-d6) δ10.75(s, 1H), 9.72(s, 1H), 8.44(d, J=4.00Hz, 1H), 8.22(s, 1H), 7.75(d, J= 8.40Hz, 2H), 7.67(d, J=8.00Hz, 2H), 7.42(d, J=7.60Hz, 1H), 7.26(d, J=8.00Hz, 1H), 7.18(d, J=9.20Hz , 2H), 7.07(d, J=1.60Hz, 1H), 7.01(t, J=7.60Hz, 1H), 6.92(t, J=7.60Hz, 1H), 6.79(d, J=8.80Hz, 2H), 4 .15-4.11(m, 1H), 3.72(t, J=4.80Hz, 4H), 3.08-2.99(m, 5H), 2.88-2.82(m, 3H), 2.78(d, J=4.40Hz, 3H) (S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(naphthalen-2-yl)propanamide 1H-NMR (400MHz, DMSO-d6) δ9.64(s, 1H), 8.27(s, 1H), 7.89-7.84(m, 2H), 7.75(t, J =4.60Hz, 1H), 7.50-7.46(m, 4H), 7.33(d, J=4.20Hz, 2H), 7.17(d, J=8.80Hz, 2H), 7 .09(d, J=8.40Hz, 2H), 7.82(d, J=9.20Hz, 2H), 4.17-4.14(m, 1H), 3.72(t, J=4.60 Hz, 4H), 3.40-3.34(m, 1H), 3.18-3.13(m, 1H), 3.02(t, J=5.00Hz, 4H), 2.24(s, 3H) (S)-Tartyl 3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-ylcarbamate 1 H-NMR (400MHz, DMSO-d6) δ10.80(s, 1H), 9.80(s, 1H), 7.64(d, J=8.00Hz, 1H), 7.45(d, J=9.20Hz, 2H), 7.32(d, J=8.40Hz, 1H), 7.15(s, 1H), 7 .05(t, J=7.40Hz, 1H), 6.97(t, J=7.20Hz, 2H), 6.90-6.84(m, 3H), 4.34-4.33(m, 1H), 3.73(t, J=4.80Hz, 4H), 3.13-2.95(m, 6H), 1.32(s, 9H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoic acid 1 H-NMR (400MHz, DMSO-d6) δ10.77(s, 1H), 8.12(d, J=8.00Hz, 1H), 7.45(d, J=4.00Hz, 2H), 7.25(t, J=12.00Hz, 2H), 7.1 2(d, J=16.40Hz, 2H), 6.96-7.01(m, 2H), 6.88(t, J=11.80Hz, 1H), 3.86(m, 1H), 3.03(m, 1H), 2.83(m, 1H), 2.30(s, 3H) (S)-Tartyl 4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-methoxyphenyl)piperazine-1-carboxylate 1 H-NMR (400MHz, CDCl3) δ8.42(s, 1H), 8.36(s, 1H), 8.11(d, J=8.80Hz, 1H), 7.48(d, J=8.00Hz, 2H), 7.3 3(d, J=8.00Hz, 1H), 7.28(d, J=8.40Hz, 1H), 7.14(t, J=7.60Hz, 1H), 7.02-6.96(m, 2H), 6.92(d, J=2.4 0Hz, 1H), 6.45(dd, J=2.40, 9.20Hz, 1H), 6.41(d, J=2.40Hz, 1H), 5.25(d, J=6.40Hz, 1H), 4.14-4.05(m , 1H), 3.57(t, J=5.20Hz, 4H), 3.20(d, J=6.80Hz, 2H), 3.05(t, J=4.80Hz, 4H), 2.28(s, 6H), 1.48(s, 9H) (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4(piperazin-1-yl)phenyl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.69(s, 1H), 8.97(s, 1H), 7.50(d, J=9.20Hz, 1H), 7.40(d, J=7.60H) z, 2H), 7.35(d, J=8.00Hz, 1H), 7.26(d, J=7.60Hz, 1H), 7.08(d, J=2.00Hz, 1H), 7.03-7.00(m, 3 H), 6.90(d, J=7.40Hz, 1H), 6.56(d, J=2.40Hz, 1H), 6.38(dd, J=2.60, 8.60Hz, 1H), 4.12-4.09( m, 2H), 3.77(s, 3H), 3.10-3.05(m, 1H), 3.01(t, J=4.80Hz, 4H), 2.85-2.79(m, 5H), 2.24(s, 3H) (S)-Tartyl 4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)phenyl)piperazine-1-carboxylate 1 H-NMR (400MHz, CDCl3) δ8.28(s, 1H), 8.02(s, 1H), 7.46(d, J=8.40Hz, 2H), 7.30(d, J=8.80Hz, 2 H), 7.24(d, J=7.20Hz, 2H), 7.16(t, J=7.20Hz, 1H), 7.04(d, J=8.00Hz, 2H), 6.98(t, J=7.40Hz, 1 H), 6.93(d, J=2.40Hz, 1H), 6.82(d, J=9.20Hz, 2H), 5.19(d, J=5.60Hz, 1H), 4.01-4.00(m, 1H), 3 .56(t, J=5.20Hz, 4H), 3.18(d, J=6.00Hz, 2H), 3.05(t, J=4.80Hz, 4H), 2.31(s, 3H), 1.48(s, 9H) (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-morpholinophenyl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (400MHz, CDCl3) δ8.37(s, 1H), 8.13(d, J=8.80Hz, 1H), 8.02(s, 1H), 7.53(d, J=8.00Hz, 2H), 7.36(d, J =8.00Hz, 1H), 7.32(d, J=8.40Hz, 1H), 7.18(t, J=7.60Hz, 1H), 7.08(d, J=8.40Hz, 2H), 7.02(t, J=7.00Hz, 1H) ), 6.96 (d, J=2.40Hz, 1H), 6.47 (dd, J=2.40, 8.80Hz, 1H), 6.41 (d, J=2.40Hz, 1H), 5.08 (d, J=6.40Hz, 1H), 4. 14-4.05(m, 1H), 3.86(t, J=4.60Hz, 4H), 3.73(s, 3H), 3.29-3.14(m, 2H), 3.11(t, J=4.80Hz, 4H), 2.32(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(piperazin-1-yl)phenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.76(s, 1H), 9.63(s, 1H), 7.51(d, J=8.40Hz, 2H) , 7.40(d, J=7.60Hz, 1H), 7.28(d, J=8.40Hz, 1H), 7.17(d, J=8.80Hz, 2H), 7.10 -7.01(m, 4H), 6.92(t, J=7.20Hz, 1H), 6.79(d, J=9.20Hz, 2H), 4.08-4.05(m, 2 H), 3.05-3.00(m, 1H), 2.95(t, J=4.80Hz, 4H), 2.85-2.79(m, 5H), 2.23(s, 3H) (S)-3-(1-formyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ9.86(s, 1H), 9.14(s, 1H), 8.23(s, 1H), 8.15(s, 1H), 7.60-7.43(m, 2H), 7.37-7.28(m, 6H), 6.95(d, 2H) (S)-3-(1H-indol-3-yl)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (400MHz, CDCl3) δ9.42(s, 1H), 8.28(d, J=1.60Hz, 1H), 7.73-7.70(m, 2H), 7.42(d, J=8.40Hz, 2H), 7.22(t, J=7.60Hz, 1H), 7.12(t , J=7.60Hz, 1H), 6.97-6.90(m, 6H), 6.65(s, 1H), 5.39(d, J=6.00Hz, 1H), 4.15-4.09(m, 1H), 3.83(s, 3H), 3.26-3.08(m, 2H), 2.25(s, 3H) (S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoate 1 H-NMR (400MHz, CDCl3) δ8.06(brs, 1H), 7.57(d, J=8.20Hz, 2H), 7.42(d, J=8.20Hz, 1H), 7.25-7.33(m, 4H), 7.08-7.18(m, 3H), 6.99-7.07 (m, 3H), 6.84(d, J=2.30Hz, 1H), 5.24(d, J=9.00Hz, 1H), 4.74-4.83(m, 2H), 4.29(td, J=5.60, 9.00Hz, 1H), 3.17-3.27(m, 2H), 2.34(s, 3H) (S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate 1 H-NMR (400MHz, CDCl3) δ7.95(brs, 1H), 7.52-7.60(m, 3H), 7.33-7.38(m, 3H), 7.27-7.32(m, 2H), 7.16-7.21(m, 3H), 7.06(t, J=7.43H) z, 1H), 6.75(d, J=2.35Hz, 1H), 6.64(d, J=7.83Hz, 1H), 5.17-5.23(m, 1H), 5.14(d, J=7.04Hz, 2H), 3.44(d, J=5.09Hz, 2H), 2.37(s, 3H) (S)-N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)-4-methylbenzamide 1 H-NMR (400MHz, CDCl3) δ8.10(brs, 1H), 7.84(d, J=7.83Hz, 1H), 7.64(d, J=8.22Hz, 2H), 7.38(d, J=8.22Hz, 1H), 7.15-7.24(m, 5H), 7.14(d , J=2.35Hz, 1H), 7.03(d, J=7.43Hz, 1H), 6.78-6.82(m, 2H), 5.06(dt, J=5.09, 7.83Hz, 1H), 3.82-3.86(m, 4H), 3.57(dd, J=5.09, 14.48, 4H) (S)-3-Hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.39(s, 1H), 7.79(d, J=8.40Hz, 2H), 7.33-7.38(m, 4H), 6.87(d, J=9.20Hz, 2H), 5.69(s, 1H), 4.11(d , J=10.40Hz, 1H), 3.85-3.87(m, 5H), 3.49-3.50(m, 1H), 3.36-3.39(m, 1H), 3.12(t, J=5.00Hz, 4H), 2.43(s, 3H), 2.30(s, 1H) (S)-3-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide 1 H-NMR (400MHz, DMSO-d6) δ9.56(s, 1H), 7.81(s, 1H), 7.62(d, J=8.00Hz, 2H), 7.20(d, J=8.40Hz, 2H), 7.13(d, J=8.80Hz, 2H), 6.81( d, J=8.80Hz, 2H), 3.71(t, J=4.80Hz, 4H), 3.53(d, J=7.60Hz, 1H), 3.00(t, J=4.60Hz, 4H), 1.81-1.86(m, 1H), 0.82(q, J=6.10Hz, 6H) (S)-1-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-3-phenylurea 1H-NMR (400MHz, DMSO-d6) δ10.90(s, 1H), 8.72(s, 1H), 7.53(d, J=7.60Hz, 1H), 7.36(t, J=8.20Hz, 3H), 7.22-7.17(m, 3H), 7.0 6(d, J=3.40Hz, 1H), 7.00-6.89(m, 2H), 6.59(d, J=8.00Hz, 1H), 4.96(d, J=6.00Hz, 1H), 3.45-3.42(m, 2H), 3.26-3.04(m, 8H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.78(s, 1H), 9.71(s, 1H), 8.12(s, 1H), 8.00(d, J=2.40Hz, 1H), 7.53(d, J= 8.00Hz, 2H), 7.45(dd, J=2.40, 9.20Hz, 1H), 7.40(d, J=8.00Hz, 1H), 7.29(d, J=7.60Hz, 1H), 7.12(d, J =7.60Hz, 2H), 7.08(d, J=2.00Hz, 1H), 7.04(t, J=7.40Hz, 1H), 6.92(t, J=7.40Hz, 1H), 6.74(d, J=9.20 Hz, 1H), 4.06(s, 1H), 3.68(t, J=4.80Hz, 4H), 3.34-3.33(m, 4H), 3.07-3.01(m, 1H), 2.88-2.82(m, 1H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(2-morpholinopyrimidin-5-yl)propanamide 1H-NMR (400MHz, DMSO-d6) δ10.80(s, 1H), 9.75(s, 1H), 8.19(s, 1H), 8.15(s, 2H) , 7.54(d, J=8.40Hz, 2H), 7.40(d, J=8.00Hz, 1H), 7.30(d, J=8.00Hz, 1H), 7.15(d , J=8.40Hz, 1H), 7.09(s, 1H), 7.04(t, J=7.40Hz, 1H), 6.93(t, J=7.40Hz, 1H), 4. 04(m, 1H), 3.62-3.61(m, 8H), 3.08-3.02(m, 1H), 2.91-2.85(m, 1H), 2.23(s, 3H) (S)-2-(4-cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.72(s, 1H), 9.85(s, 1H), 8.57(s, 1H), 7.57(s, 4H), 7.48(d, J=7.60Hz, 1H), 7.29-7.23(m, 3H), 7.0 7-7.01(m, 2H), 6.93(t, J=7.20Hz, 1H), 6.86(d, J=8.80Hz, 2H), 4.12(s, 1H), 3.73(s, 4H), 3.04-3.00(m, 3H), 2.90-2.84(m, 1H) (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanamide 1 H-NMR (400MHz, DMSO-d6) δ10.76(s, 1H), 9.92(s, 1H), 8.87(s, 1H), 8.81(s, 1H), 8.0(d, J=8.40Hz, 1H), 7.60(d, J=8.00Hz, 1H), 7.52(d, J=7.60Hz, 1H), 7.22-7.1 9(m, 3H), 7.12(d, J=1.60Hz, 1H), 7.01(d, J=7.40Hz, 1H), 6.92(d, J=7.40Hz, 1H) , 6.82(d, J=9.20Hz, 2H), 4.21(m, 1H), 3.73(t, J=4.40Hz, 4H), 3.08-2.90(m, 6H) (S)-Methyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate 1 H-NMR (400MHz, CDCl3) δ8.16(s, 1H), 7.74(d, J=8.40Hz, 2H), 7.27-7.25(m, 4H), 6.83(d, J=8.80Hz, 2H), 6.21(d, J=7.20Hz, 1H ), 3.9-3.84(m, 5H), 3.69(s, 3H), 3.10(t, J=4.60Hz, 4H), 2.58-2.50(m, 1H), 2.36(s, 3H), 2.32-2.25(m, 1H), 2.05-1.93(m, 2H) (S)-3-(1H-benzo[d]imidazol-1-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.97(s, 1H), 7.68(s, 1H), 7.57(d, J=7.60Hz, 2H), 7.38(d, J=8.00Hz, 1H), 7.27(d, J=8.00Hz, 1H), 7.12- 7.00(m, 6H), 6.72(d, J=8.80Hz, 2H), 4.49(s, 2H), 4.44-4.43(m, 1H), 3.80(t, J=4.60Hz, 4H), 3.03(t, J=4.60Hz, 4H), 2.24(s, 3H) (R)-3-(2,3-dioxo-3,4-dihydroquinoxalin-1(2H)-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, CDCl3) δ7.48(d, J=8.80Hz, 2H), 7.43(d, J=7.60Hz, 2H), 7.37(d, J=8.00Hz, 1H), 7.32(s, 1H), 7.27-7.20(m, 2H), 7.07(d, J=7.20Hz, 1H), 6.91(t, J=6.60Hz, 4H), 4.75-4.68(m, 1H), 4.32(d, J=12.4Hz, 2H), 3.87(s, 4H), 3.14(s, 4H), 2.26(s, 3H) (S)-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)-5-(trifluoromethyl)picolinamide 1 H-NMR (400MHz, CDCl3) δ8.82(s, 1H), 8.35(d, J=8.00Hz, 1H), 8.22(s, 1H), 8 .13(d, J=8.00Hz, 1H), 7.71(d, J=8.00Hz, 2H), 7.28-7.25(m, 2H), 7.19(d, J =8.40Hz, 2H), 6.81(d, J=8.80Hz, 2H), 3.85(t, J=4.80Hz, 4H), 3.80-3.76(m , 1H), 3.45-3.39(m, 2H), 3.09(t, J=4.60Hz, 4H), 2.31(s, 3H), 1.87-1.73(m, 2H), 1.60-1.55(m, 2H), 1.33-1.30(m, 2H) (S)-Benzyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate 1H-NMR (400MHz, CDCl3) δ8.25(s, 1H), 7.71(d, J=8.00Hz, 2H), 7.36-7.30(m, 5H), 7.21(d, J=8.80 Hz, 2H), 7.16(d, J=8.00Hz, 2H), 6.77(d, J=8.80Hz, 2H), 6.30(d, J=7.60Hz, 1H), 5.12-5.04(m, 2H), 3.95-3.90(m, 1H), 3.83(t, J=4.60Hz, 4H), 3.06(t, J=4.80Hz, 4H), 2.55-2.48(m, 1H), 2.36-2.30(m, 1H), 2.28(s, 3H), 2.06-2.03(m, 1H), 1.96-1.93(m, 1H) (S)-Benzyl 3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoate 1 H-NMR (400MHz, CDCl3) δ8.39(s, 1H), 7.75(d, J=8.00Hz, 2H), 7.33-7.23(m, 9H), 6.81(d, J=8.80Hz, 2H), 6.25(d, J=8.80Hz, 1H), 5.09-5.00(m, 2 H), 4.22-4.21(m, 1H), 3.84(t, J=4.80Hz, 4H), 3.08(t, J=4.80Hz, 4H), 3.03(dd, J=4.00, 17.2Hz, 1H), 2.41(dd, J=6.20, 17.4Hz, 1H), 2.36(s, 3H) (S)-4-Methyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide 1H-NMR (400MHz, CDCl3) δ8.73(s, 1H), 7.69(d, J=8.00Hz, 2H), 7.42(d, J=8.00Hz, 2H), 7.22(d, J=8.80Hz, 2H), 6.84-6.80(m, 3H) 4.90-4.86(m, 1H), 3.84(t, J=4.80Hz, 4H), 3.08(t, J=4.80Hz, 4H), 2.39(s, 3H), 1.90-1.88( m, 1H), 1.86-1.71(m, 2H), 0.97(d, J=6.40Hz, 3H), 0.90(d, J=6.40Hz, 3H) 2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)acetamide 1 H-NMR (400MHz, CDCl3) δ7.96(s, 1H), 7.76(d, J=8.40Hz, 2H), 7.35-7.32(m, 4H), 6.85(d, J=8.80Hz, 2H), 5 .31(t, J=6.80Hz, 1H), 3.85(t, J=4.80Hz, 4H), 3.69(d, J=6.40Hz, 2H), 3.11(t, J=4.80Hz, 4H), 2.42(s, 3H) (S)-3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoic acid 1 H-NMR (400MHz, DMSO-d6) δ9.77(s, 1H), 7.65-7.20(m, 4H), 7.21(d, J=4.00Hz, 2H), 6.82(d, J=8.80Hz, 2H), 4.17(t, J=7.00Hz, 1H), 3.72(t, J=4.40Hz, 4H), 3.02(t, J=4.60Hz, 4H), 2.57(dd, J=16.2, 6.60Hz, 1H), 2.35(dd, J=16.0, 7.60Hz, 1H), 2.25(s, 3H) (S)-4-(4-Methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoic acid 1H-NMR (400MHz, DMSO-d6) δ9.67(s, 1H), 7.65(d, J=8.40Hz, 2H), 7.25(d, J=7.60Hz, 2H), 7.19(d, J=8.80Hz, 2H), 6.84(d, J=8.4 0Hz, 2H), 3.83-3.79(m, 1H), 3.72(t, J=4.60Hz, 4H), 3.02(t, J=4.80Hz, 4H), 2.26(s, 3H), 2.20-2.11(m, 2H), 1.80-1.70(m, 2H) (S)-3-(4-hydroxyphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ9.61(s, 1H), 9.18(s, 1H), 8.05(s, 1H), 7.49(d, J =8.00Hz, 2H), 7.15(d, J=8.40Hz, 4H), 6.93(d, J=7.60Hz, 2H), 6.82(d, J=9. 20Hz, 2H), 6.57(d, J=8.80Hz, 2H), 3.98-3.85(m, 1H), 3.72(t, J=4.60Hz, 4H ), 3.01(t, J=4.60Hz, 4H), 2.78-2.73(m, 1H), 2.67-2.59(m, 1H), 2.33(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenylpropanamide 1 H-NMR (400MHz, CDCl3) δ8.14(s, 1H), 8.10(s, 1H), 7.45(d, J=8.40Hz, 2H), 7.34(d, J=7.60Hz, 2H), 7.30-7.24(m, 4H), 7.1 7-7.11(m, 2H), 7.09-6.92(m, 3H), 6.91(s, 1H), 5.19(d, J=5.60Hz, 1H), 4.05-4.01(m, 1H), 3.20-3.17(m, 2H), 2.29(s, 3H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenylpropanamide 1H NMR(400 MHz, DMSO-d6)δ10.78(s, 1H), 9.98(s, 1H), 8.40(s, 1H), 7.40-7.39(m, 5H), 7.36(d, J=8.40Hz, 2H), 7.30-7.23(m, 3H), 7.10(s, 1H), 7.06-7.01(m, 2H), 6.93(t, J=7.20Hz, 1H), 4.16-4.13(m, 1H), 3.05(dd, J=14.2, 6.00Hz, 1H), 2.87(dd, J=14.7, 8.00Hz, 1H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(thiophen-2-ylmethyl)propanamide 1 H-NMR (400MHz, CDCl3) δ8.20(s, 1H), 7.41(d, J=8.40Hz, 2H), 7.28-7.24(m, 2H), 7.16-7.11(m, 2H), 7.01-6.88(m, 3H), 6.87(s , 1H), 6.81(s, 1H), 6.74(s, 1H), 5.13(d, J=6.00Hz, 1H), 4.48-4.45(m, 2H), 3.94-3.91(m, 1H), 3.11-3.09(m, 2H), 2.31(s, 3H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiophen-2-ylmethyl)propanamide 1 6 .94-6.88(m, 2H), 6.86(d, J=2.40Hz, 1H), 4.30-4.26(m, 2H), 3.99-3.95(m, 1H), 2.99(dd, J=14.2, 6.00Hz, 1H), 2.80(dd, J=14.7, 8.00Hz, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(2-methoxyphenyl)thiazol-2-yl)propanamide 1 H-NMR (400MHz, DMSO-d6) δ12.39(s, 1H), 10.76(s, 1H), 8.48(s, 1H), 7.64(s, 1H), 7.47(d, J=7.60Hz, 1H), 7.41-7.11(m , 6H), 7.08-7.01(m, 5H), 6.91(t, J=7.60Hz, 1H), 4.34-4.30(m, 1H), 3.91(s, 3H), 3.12-3.07(m, 1H), 2.91-2.85(m, 1H) (S)-N-(3-(N-(4-methyl-1-morpholino-1-oxopentan-2-yl)sulfamoyl)phenyl)acetamide 1 H-NMR (400MHz, CDCl3) δ8.47(s, 1H), 8.25(d, J=8.80Hz, 1H), 7.76(t, J=1.80Hz, 1H ), 7.54(d, J=7.60Hz, 1H), 7.45(t, J=8.00Hz, 1H), 6.69(d, J=9.60Hz, 1H), 4.15-4. 08(m, 1H), 3.59-3.49(m, 2H), 3.42-3.18(m, 6H), 2.16(s, 3H), 1.99-1.94(m, 1H), 1 .52-1.45(m, 1H), 1.18-1.11(m, 1H), 0.95(d, J=6.80Hz, 3H), 0.91(d, J=6.80Hz, 3H) (S)-Benzyl 4-methyl-2-(3-phenylureido)pentanoate 1 H-NMR (400MHz, CDCl3) δ7.38(s, 1H), 7.34-7.01(m, 8H), 6.99-6.97(m, 1H), 5.83(d, J=8.00Hz, 1H), 5.19-5.07( m, 2H), 4.65-4.60(m, 1H), 1.71-1.57(m, 2H), 1.51-1.46(m, 1H), 0.91(d, J=6.40Hz, 3H), 0.88(d, J=6.40Hz, 3H) 4-Methyl-N-(2-morpholino-2-oxoethyl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.76 (d, J=8.00Hz, 2H), 7.30 (d, J=8.00Hz, 2H), 6.20 (t, J=4.60Hz, 1H), 3. 79(d, J=4.80Hz, 2H), 3.58-3.62(m, 4H), 3.51(t, J=4.40Hz, 2H), 3.32(t, J=4.60Hz, 2H), 2.4(s, 3H) 4-Methyl-N-(1-(morpholine-4-carbonyl)cyclohexyl)benzenesulfonamide 1 H-NMR (400MHz, CDCl3) δ7.79(d, J=8.00Hz, 2H), 7.29(d, J=8.00Hz, 2H), 5.33( s, 1H), 3.74-3.78(m, 8H), 2.43(s, 3H), 1.74-1.91(m, 4H), 1.17-1.40(m, 6H).

[0053] (S)-4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoic acid 1 H-NMR (400MHz, CDCl3) δ8.20(d, J=8.40Hz, 2H), 7.94(d, J=8.40Hz, 2H), 6.49(d, J=9.20Hz, 1H), 4.46-4.41( m, 1H), 3.84-3.78(m, 2H), 3.65-3.25(m, 14H), 1.93-1.89(m, 1H), 1.56-1.36(m, 2H), 0.91(t, J=7.00Hz, 6H) (S)-2-(4-hydroxyphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, DMSO-d6) δ10.78(s, 1H), 10.18(s, 1H), 9.64(s, 1H), 7.84(d, J=8.40Hz, 1H), 7.50 (d, J=8.80Hz, 2H), 7.39(d, J=7.60Hz, 1H), 7.29(d, J=7.60Hz, 1H), 7.22(d, J=9.20Hz, 2H), 7.06( d, J=2.40Hz, 1H), 7.03(d, J=7.20Hz, 1H), 6.93(t, J=7.40Hz, 1H), 6.82(d, J=9.20Hz, 2H), 6.70(d , J=8.40Hz, 2H), 4.08-4.02(m, 1H), 3.72(t, J=4.80Hz, 4H), 3.07-3.00(m, 5H), 2.84-2.79(m, 1H) (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoic acid 1 H-NMR (400MHz, DMSO-d6) δ10.77(s, 1H), 9.83(s, 1H), 8.43(d, J=9.20Hz, 1H), 7. 76(d, J=8.00Hz, 2H), 7.63(d, J=8.40Hz, 2H), 7.44(d, J=7.60Hz, 1H), 7.26-7.22 (m, 3H), 7.09(d, J=2.04Hz, 1H), 7.00(t, J=7.20Hz, 1H), 6.91(t, J=7.60Hz, 3H), 4.14-4.12(m, 1H), 3.76(t, J=4.60Hz, 4H), 3.07-3.03(m, 5H), 2.90-2.86(m, 1H) (S)-2-Amino-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide 1H-NMR (400MHz, CDCl3) δ9.27(s, 1H), 8.21(s, 1H), 7.70(d, J=8.00Hz, 1H), 7.51-7.47(m, 2H), 7.37(d, J=8.40Hz, 1H), 7.22-7.11(m, 2H), 7.08(d, J=2.40Hz, 1H), 6.89-6.86(m, 2H), 3.86-3.82(m, 5H), 3.49-3.45(m, 1H), 3.11(t, J=4.80Hz, 4H), 3.04-2.99(m, 1H), 1.81(s, 2H) (S)-N-(4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (400MHz, CDCl3) δ8.54(s, 1H), 8.49(s, 1H), 8.12(d, J=8.40Hz, 1H), 7.46(d, J=8. 40Hz, 2H), 7.32-7.26(m, 2H), 7.13(t, J=7.60Hz, 1H), 7.00-6.95(m, 3H), 6.92(d, J=2.40 Hz, 1H), 6.45-6.40(m, 2H), 5.37(d, J=5.60Hz, 1H), 4.09-4.05(m, 1H), 3.75(t, J=5.40H) z, 2H), 3.71(s, 3H), 3.59(t, J=5.00Hz, 2H), 3.21-3.04(m, 6H), 2.28(s, 3H), 2.13(s, 3H) (S)-N-(4-(4-acetylpiperazin-1-yl)phenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (400MHz, CDCl3) δ8.31(s, 1H), 8.11(s, 1H), 8.47(d, J=8.40Hz, 2H), 7.31-7.25(m, 5H), 7.16( t, J=7.60Hz, 1H), 7.04(d, J=8.40Hz, 2H), 6.99(t, J=7.60Hz, 1H), 6.94(d, J=2.40Hz, 1H), 6.82(d, J= 9.20Hz, 2H), 5.22(d, J=6.00Hz, 1H), 4.02-4.00(m, 1H), 3.74(t, J=5.00Hz, 2H), 3.59(t, J=5.00Hz, 2 H), 3.18(d, J=6.40Hz, 2H), 3.10(t, J=5.00Hz, 2H), 3.05(t, J=5.00Hz, 2H), 2.31(s, 3H), 2.12(s, 3H) (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-morpholinobenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (400MHz, DMSO-d6) δ10.71(s, 1H), 10.17(s, 2H), 7.99(s, 1H), 7.82(d, J=8.8 0Hz, 2H), 7.37(d, J=8.00Hz, 1H), 7.33(d, J=8.40Hz, 2H), 7.26(d, J=7.26Hz, 1H), 7 .14(s, 1H), 7.04-6.98(m, 5H), 6.90(t, J=7.40Hz, 1H), 4.07(s, 1H), 3.74(t, J=4.4 0Hz, 4H), 3.24(t, J=4.80Hz, 4H), 3.11-3.06(m, 1H), 2.80-2.74(m, 1H), 2.21(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)propanamide 1H-NMR (400MHz, DMSO-d6) δ12.24(s, 1H), 10.76(s, 1H), 8.21(s, 1H), 7.73(d, J=8.8 0Hz, 2H), 7.46(d, J=8.00Hz, 2H), 7.41(d, J=8.00Hz, 1H), 7.35(s, 1H), 7.27(d, J=8 .40Hz, 1H), 7.05-6.97(m, 6H), 6.91(t, J=7.60Hz, 1H), 4.29(s, 1H), 3.74(t, J=4.6 0Hz, 4H), 3.15(t, J=4.60Hz, 4H), 3.10-3.05(m, 1H), 2.88-2.82(m, 1H), 2.18(s, 3H) (S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate 1 H-NMR (400MHz, DMSO-d6) δ12.39(s, 1H), 10.77(s, 1H), 8.25(d, J=8.00Hz, 1 H), 8.02(s, 4H), 7.81(s, 1H), 7.46(d, J=8.40Hz, 2H), 7.42(d, J=8.00Hz, 1H) ), 7.27(d, J=8.40Hz, 1H), 7.06-7.01(m, 4H), 6.91(t, J=7.60Hz, 1H), 4.32- 4.30(s, 1H), 3.86(s, 3H), 3.12-3.06(m, 1H), 2.90-2.84(m, 1H), 2.17(s, 3H) (S)-Benzyl 3-(1H-indol-3-yl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanoate 1H-NMR (400MHz, CDCl3) δ8.85(d, J=1.60Hz, 1H), 7.91(s, 1H), 7.83(dd, J=1.60, 8.40Hz, 1H), 7.42(d, J=8.40Hz, 1H), 7.36-7.33(m, 4H), 7.26-7.1 5(m, 5H), 7.08-7.04(m, 1H), 6.84(d, J=2.40Hz, 1H), 5.40(d, J=8.80Hz, 1 H), 5.03(s, 2H), 4.43-4.38(m, 1H), 3.33-3.28(m, 1H), 3.16-3.10(m, 1H) (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5 -(4-nitrophenyl)pentanediamide 1 H-NMR (400MHz, DMSO-d6) δ10.57(s, 1H), 9.71(s, 1H), 8.21(d, J=8.80Hz, 2H ), 8.08(s, 1H), 7.81(d, J=9.20Hz, 2H), 7.65(d, J=8.40Hz, 2H), 7.22-7.18(m , 4H), 6.84(d, J=8.80Hz, 2H), 3.86(t, J=6.80Hz, 1H), 3.72(t, J=4.60Hz, 4H ), 3.02(t, J=4.80Hz, 4H), 2.46-2.37(m, 2H), 2.21(s, 3H), 1.93-1.79(m, 2H) (S)-Benzyl 5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexylcarbamate 1 H-NMR (400MHz, CD3OD) δ7.71(d, J=8.00Hz, 2H), 7.32-7.25(m, 5H), 7.22(d, J=8.40Hz, 2H), 7.15(d, J=8.40Hz, 2H), 6.86 (d, J=9.20Hz, 2H), 5.06(s, 2H), 3.82-3.78(m, 5H), 3.07-3.03(m, 6H), 2.26(s, 3H), 1.69-1.59(m, 2H), 1.48-1.28(m, 4H) (S)-6-Amino-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)hexanamide 1 H-NMR (400MHz, DMSO-d6) δ9.65(s, 1H), 7.65(d, J=8.40Hz, 2H), 7.25-7.19(m, 4H), 6.83(d, J=8.80Hz, 2H), 3.77 -3.71(m, 5H), 3.02(t, J=4.80Hz, 4H), 2.42(t, J=6.40Hz, 2H), 2.26(s, 3H), 1.52-1.44(m, 2H), 1.24-1.12(m, 4H) (S)-3,5-Dimethoxy-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)benzamide 1 H-NMR (400MHz, CDCl3) δ8.60(s, 1H), 7.68(d, J=8.00Hz, 2H), 7.25(d, J=8.80Hz, 2H), 7.14(d, J=8.40Hz, 2H), 6.98(d, J=2.40Hz, 2H), 6.77(d, J=9.20Hz, 2H), 6.86(t, J=6.00Hz, 1H), 6.58( s, 1H), 6.35(d, J=7.20Hz, 1H), 3.83(t, J=4.60Hz, 4H), 3.78-3.75(m, 7H), 3.39-3.32(m, 2H), 3.06(t, J=4.80Hz, 4H), 2.26(s, 3H), 1.85-1.71(m, 2H), 1.52-1.47(m, 2H), 1.30-1.23(m, 2H) (S)-N 5 -(4-Methoxybenzyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide 1H-NMR (400MHz, DMSO-d6) δ9.60(s, 1H), 8.25(t, J=5.80Hz, 1H), 7.95(s, 1H), 7 .64(d, J=8.40Hz, 2H), 7.23(d, J=8.40Hz, 2H), 7.19(d, J=9.20Hz, 2H), 7.14(d, J=8.80Hz, 2H), 6.84(t, J=8.80Hz, 4H), 4.15(d, J=6.00Hz, 2H), 3.82-3.71(m, 8H), 3.02(t, J=4.80Hz, 4H), 2.26(s, 3H), 2.17-2.05(m, 2H), 1.82-1.75(m, 2H) (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5 -Phenylpentanediamide 1 H-NMR (400MHz, DMSO-d6) δ9.89(s, 1H), 9.64(s, 1H), 7.98(s, 1H), 7.66(d, J =8.00Hz, 2H), 7.56(d, J=8.40Hz, 2H), 7.28-7.19(m, 6H), 7.01(t, J=7.40Hz , 1H), 6.84(d, J=8.80Hz, 2H), 3.86(t, J=6.80Hz, 1H), 3.72(t, J=4.60Hz, 4H ), 3.02(t, J=4.60Hz, 4H), 2.41-2.26(m, 2H), 2.23(s, 3H), 1.94-1.80(m, 2H) (S)-2-(4-methylphenylsulfonamido)-5-morpholino-N-(4-morpholinophenyl)-5-oxopentanamide 1H-NMR (400MHz, CDCl3) δ8.75(s, 1H), 7.74(d, J=8.40Hz, 2H), 7.34(d, J=8.80Hz, 2H ), 7.28(d, J=8.00Hz, 2H), 7.11(d, J=6.00Hz, 1H), 8.65(d, J=8.80Hz, 2H), 3.86(t, J=4.60Hz, 1H), 3.78-3.65(m, 6H), 3.59-3.55(m, 1H), 3.45-3.33(m, 2H), 3.10(t, J =5.00Hz, 4H), 2.64-2.63(m, 2H), 2.38(s, 3H), 2.23-2.18(m, 2H), 2.07-2.02(m, 2H) (S)-N 5 -(4-fluorophenyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide 1 H-NMR (400MHz, DMSO-d6) δ9.99(s, 1H), 9.68(s, 1H), 8.04(s, 1H), 7.65(d, J=8.00Hz, 2H), 7.58-7.55(m, 2H), 7.21(t, J=8.00Hz, 4H), 7. 12(t, J=8.80Hz, 2H), 6.84(d, J=8.80Hz, 2H), 3.85(s, 1H), 3.72(s, 4H), 3.02(s, 4H), 2.38-2.26(m, 2H), 2.22(s, 3H), 1.89-1.81(m, 2H) (S)-N 5 -(4-tert-butylphenyl)-2-(4-methylphenylsulfonamide)-N 1 -(4-morpholinophenyl)pentanediamide 1H-NMR (400MHz, DMSO-d6) δ9.86(s, 1H), 9.69(s, 1H), 8.05(s, 1H), 7.65(d, J=8. 40Hz, 2H), 7.47(d, J=8.80Hz, 2H), 7.29(d, J=8.80Hz, 2H), 7.22-7.19(m, 4H), 6 .84(d, J=8.80Hz, 2H), 3.84(t, J=6.80Hz, 1H), 3.73(t, J=4.60Hz, 4H), 3.02(t, J=4.80Hz, 4H), 2.40-2.25(m, 2H), 2.22(s, 3H), 1.92-1.77(m, 2H), 1.24(s, 9H) (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 5 -(4-(trifluoromethyl)phenyl)pentanediamide 1 H-NMR (400MHz, DMSO-d6) δ10.30(s, 1H), 9.69(s, 1H), 8.05(s, 1H), 7.77(d, J=8.80Hz, 2H), 7.65(d, J=8.00Hz, 4H), 7.22-7. 19(m, 4H), 6.84(d, J=8.80Hz, 2H), 3.86(s, 1H), 3.72(s, 4H), 3.02(s, 4H), 2.44-2.33(m, 2H), 2.21(s, 3H), 1.93-1.82(m, 2H) (S)-2-(4-Methylphenylsulfonamide)-N 1 -(4-Morpholinophenyl)-N 4 -(4-Nitrophenyl)succinic acid amide 1H-NMR (400MHz, DMSO-d6) δ10.55(s, 1H), 9.80(s, 1H), 8.21(d, J=8.80Hz, 2H), 8.18(s, 1H) , 7.75(d, J=9.20Hz, 2H), 7.65(d, J=8.40Hz, 2H), 7.25(d, J=8.80Hz, 2H), 7.18(d, J=8.40H z, 2H), 6.84(d, J=8.80Hz, 2H), 4.35(t, J=6.80Hz, 1H), 3.72(t, J=4.60Hz, 4H), 3.02(t, J= 4.80Hz, 4H), 2.78(dd, J=6.60, 15.40Hz, 1H), 2.62(dd, J=7.80, 15.40Hz, 1H), 2.21(s, 3H) (S)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, CDCl3) δ8.10(s, 1H), 7.45-7.43(d, J=10.00Hz, 2H), 7.32(s, 1H), 7.31-7.30(d, J=5.00Hz, 1H), 7.26-7.25(d, J=5.00Hz, 1H), 7.18-7.15(t, J=7.50Hz, 1H), 7.06-7.05(d, J=5.0 0Hz, 2H), 7.01-6.98(t, J=7.50Hz, 1H), 6.83(s, 1H), 6.67(s, 1H), 6.30(s, 1H), 6.15(s, 1H), 4.9 7-4.96(d, J=0.94Hz, 1H), 4.40-4.31(m, 2H), 3.93-3.90(m, 1H), 3.15-3.07(m, 2H), 2.34(s, 3H) (S)-2-(4-bromophenylsulfonamido)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)propanamide 1H-NMR (500MHz, CDCl3) δ8.64(s, 1H), 7.98(s, 3H), 7.32-7.22(m, 6H), 7.18-7.15(t, J=7.50Hz, 1H), 6.88(s, 1H) ), 6.29(s, 1H), 6.15(s, 1H), 5.69(s, 1H), 4.33(m, 2H), 3.95-3.91(m, 1H), 3.28-3.24(m, 1H), 3.05-3.00(m, 1H) (S)-3-(1H-indol-3-yl)-N-isopropyl-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, CDCl3) δ8.27(s, 1H), 7.47-7.45(d, J=10.00Hz, 2H), 7.33-7.31(d, J =10.00Hz, 2H), 7.19-7.16(t, J=7.50Hz, 1H), 7.07-7.05(d, J=10.00Hz, 2H), 7.02-6 .99(t, J=7.50Hz, 1H), 6.92(s, 1H), 6.02-6.00(d, J=10.00Hz, 1H), 5.09-5.07(d, J= 10.00Hz, 1H), 3.97-3.90(m, 1H), 3.86-3.82(m, 1H), 3.15-3.07(m, 2H), 2.33(s, 3H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-isopropylpropanamide 1 H-NMR (500MHz, MeOD) δ10.23(s, 1H), 7.97-7.95(d, J=5.00Hz, 1H), 7.50-7.48(d, J=10. 00Hz, 2H), 7.42-7.41(d, J=5.00Hz, 1H), 7.27-7.25(d, J=10.00Hz, 1H), 7.06-7.02(m, 4H) ), 6.94-6.90(m, 2H), 6.86-6.84(d, J=10.00Hz, 1H), 6.80-6.76(t, J=10.00Hz, 1H), 4.66 (s, 1H), 4.15-4.12(t, J=7.50Hz, 1H), 3.22-3.18(m, 1H), 3.03-2.99(m, 1H), 2.11(s, 3H) (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (500MHz, CDCl3) δ7.86-7.64(d, J=8.50Hz, 2H), 7.31-7.26(m, 4H), 7.11-7.08(t, J=7.50Hz, 1H), 7.04(s, 1H), 6.95-6 .91(m, 3H), 6.89-6.87(d, J=8.00Hz, 2H), 4.10-4.07(m, 1H), 3.85(s, 3H), 3.35-3.31(m, 1H), 3.04-3.00(m, 1H), 2.26(s, 3H) (S)-2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoyl)-N-(4-methoxyphenyl)hydrazinecarboxamide 1 H-NMR (500MHz, MeOD) δ7.39-7.36(t, J=7.00Hz, 4H), 7.28-7.26(d, J=8.00Hz, 1H), 7.22-7.20(d, J=7.50Hz, 1H), 7.08-7.05(t, J=7.50Hz, 1H) , 7.01(s, 1H), 6.98(s, 1H), 6.97(s, 1H), 6.89-6.84(m, 3H), 3.89-3.86 (m, 1H), 3.76(s, 3H), 3.25-3.21(m, 1H), 2.93-2.89(m, 1H), 2.30(s, 3H) (S)-4-Bromo-N-(1-(3,5-dimethyl-1H-pyrazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide 1H-NMR (500MHz, DMSO-d6) δ10.76(s, 1H), 8.65(s, 1H), 7.66-7.65(d, J=9.50Hz, 1H), 7.30- 7.27(t, J=7.50Hz, 3H), 7.16-7.15(d, J=8.00Hz, 2H), 7.10(s, 1H), 7.07-7.04(t, J=7.50H z, 1H), 6.96-6.93(t, J=7.50Hz, 1H), 6.24(s, 2H), 5.39-5.37(d, J=8.50Hz, 1H), 3.20-3.1 6(d, J=14.00, 3.00Hz, 1H), 2.89-2.84(d, J=14.00, 10.50Hz, 1H), 2.92(s, 3H), 2.27(s, 3H) (S)-N-(3-(1H-indol-3-yl)-1-oxo-1-(3-phenyl-1H-pyrazol-1-yl)propan-2-yl)-4-bromobenzenesulfonamide 1 H-NMR (500MHz, DMSO-d6) δ10.77(s, 1H), 8.86(s, 1H), 8.48(s, 1H), 8.00-7.98(d, J=7.50Hz, 2 H), 7.69-7.68(d, J=7.50Hz, 1H), 7.58-7.55(t, J=7.00Hz, 2H), 7.52-7.49(t, J=7.50Hz, 1H), 7.29-7.23(m, 4H), 7.17(s, 1H), 7.15(s, 1H), 7.11-7.04(m, 2H), 6.98-6.92(m, 1H), 5.50-5.4 9(d, J=7.00Hz, 1H), 3.28-3.25(d, J=14.00, 4.00Hz, 1H), 2.97-2.92(d, J=14.00, 10.00Hz, 1H) N-((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1H-NMR (500MHz, MeOD) δ7.33-7.32(d, J=8.00Hz, 1H), 7.25-7.20(t, J=7.50Hz, 3H), 7.06-7.03(t , J=7.50Hz, 1H), 7.00(s, 1H), 6.91-6.88(t, J=8.00Hz, 1H), 6.85-6.83(d, J=8.00Hz, 2H), 4.04- 4.01(d, J=9.50, 4.50Hz, 1H), 3.29-3.25(d, J=15.00, 5.00Hz, 1H), 2.94-2.89(d, J=15.00, 10.0 0Hz, 1H), 2.24(s, 3H), 2.02-2.01(d, J=6.00Hz, 3H), 1.95(s, 6H), 1.80-1.74(t, J=12.50Hz, 6H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(p-tolyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ12.47(s, 1H), 10.79(s, 1H), 8.53-8.52(d, J=7.50Hz, 1H), 7.78-7.77(d, J=8.00 Hz, 2H), 7.55(s, 1H), 7.48-7.47(d, J=7.50Hz, 1H), 7.44-7.37(m, 4H), 7.29-7.27(d, J=8.00Hz, 1H), 7.25- 7.23(d, J=8.50Hz, 2H), 7.09(d, J=2.50Hz, 1H), 7.06-7.03(t, J=7.50Hz, 1H), 6.94-6.91(t, J=7.50Hz, 1H) , 4.35-4.31(m, 1H), 3.12-3.08(d, J=14.50, 6.50Hz, 1H), 2.91-2.86(d, J=15.00, 10.00Hz, 1H), 2.33(s, 3H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-pentylpropanamide 1H-NMR (500MHz, CDCl3) δ8.27(s, 1H), 8.02(s, 1H), 7.47-7.46(d, J=10.00Hz, 2H), 7.32-7.31( d, J=5.00Hz, 2H), 7.28-7.25(d, J=7.50Hz, 2H), 7.23-7.22(d, J=5.00Hz, 1H), 7.20-7.17(t, J =7.50Hz, 1H), 7.08-7.01(m, 5H), 6.84(s, 1H), 6.37-6.35(t, J=5.00Hz, 1H), 5.08-5.07(d, J= 5.00Hz, 1H), 3.43-3.35(m, 2H), 3.10-3.07(t, J=7.50Hz, 2H), 2.70-2.59(m, 2H), 2.35(s, 3H) (S)-2-(4-bromophenylsulfonamido)-N-(4-(4-fluorophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, MeOD) δ7.91-7.88(m, 2H), 7.45-7.42(m, 3H), 7.32(s, 1H), 7.30-7.27(m, 3H), 7.14-7.10(t, J=10.00Hz, 2H), 7. 09-7.06(t, J=7.50Hz, 1H), 7.02(s, 1H), 6.97-6.94(t, J=7.50Hz, 1H), 4.31-4.28(m, 1H), 3.28-3.24(m, 1H), 3.08-3.03(m, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-nitrophenyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, MeOD) δ8.28-8.26(d, J=10.00Hz, 2H), 8.12-8.10(d, J=10.00Hz, 2H), 7.68(s, 1H), 7.47-7.44(m, 3H), 7.31-7. 27(m, 3H), 7.09-7.06(t, J=7.50Hz, 1H), 6.97-6.94(t, J=7.50Hz, 1H), 4.31-4.28(m, 1H), 3.29-3.25(m, 1H), 3.10-3.05(m, 1H) (S)-N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1 H-NMR (500MHz, MeOD) δ7.89-7.88(d, J=8.50Hz, 2H), 7.43-7.41(d, J=8.80Hz, 1H), 7.28-7.2 6(d, J=8.00Hz, 1H), 7.22-7.21(d, J=8.50Hz, 2H), 7.16-7.14(d, J=8.00Hz, 2H), 7.10-7.07( t, J=7.00Hz, 1H), 7.03-7.01(d, J=11.00Hz, 3H), 6.96-6.93(t, J=7.00Hz, 1H), 4.18-4.15(d , J=10.00, 5.00Hz, 1H), 3.87(s, 3H), 3.35-3.32(m, 1H), 3.00-2.95(d, J=10.50, 4.00Hz, 1H) (S)-2-(4-bromophenylsulfonamido)-N-(4-(4-cyanophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.88-2.93(dd, J=14.18, 8.80Hz, 1H), 3.09-3.13(dd, J=14.18, 6.35Hz, 1H) , 4.34-4.35(d, J=6.35Hz, 1H), 6.91-6.94(t, J=7.33Hz, 1H), 7.02-7.05(t, J=7.82Hz, 1H), 7.09-7.10( d, J=1.95Hz, 1H), 7.27-7.28(d, J=8.31Hz, 1H), 7.37-7.42(m, 4H), 7.47-7.48(d, J=7.82Hz, 1H), 7.88- 7.91(m, 3H), 8.05-8.06(d, J=8.31Hz, 2H), 8.55-8.57(d, J=7.33Hz, 1H), 10.80(s, 1H), 12.55(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.88-2.92(dd, J=14.18, 8.80Hz, 1H), 3.09-3.13(dd, J=14.18, 6.35Hz, 1H), 4.33-4 .35(m, 1H), 6.90-6.93(t, J=7.33Hz, 1H), 7.02-7.05(t, J=7.33Hz, 1H), 7.09(d, J=1.95Hz, 1H), 7.27-7.28(d, J=8.31Hz, 1H), 7.37-7.42(q, J=8.31, 8.80, 7.82Hz, 4H), 7.47-7.48(d, J=7.82Hz, 1H), 7.78-7.80(d, J=8.31H) z, 2H), 7.85(s, 1H), 8.08-8.10(d, J=8.31Hz, 2H), 8.52-8.54(d, J=7.33Hz, 1H), 10.78(s, 1H), 12.54(brs, 1H).

[0054] (S)-4-Bromo-N-(1-(2-dodecanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide 1 H-NMR (500MHz, CDCl3) δ0.86-0.89(t, J=6.84Hz, 3H), 1.26(s, 16H), 1.51-1.54(t, J=6.35Hz, 2H), 2.30-2.3 7(m, 2H), 3.13-3.17(dd, J=14.67, 7.82Hz, 1H), 3.22-3.26(dd, J=14.67, 5.86Hz, 1H), 4.36-4.38(t, J=6.84 Hz, 1H), 7.02(s, 1H), 7.06-7.09(t, J=7.33Hz, 1H), 7.18-7.21(t, J=7.33Hz, 1H), 7.32-7.34(d, J=8.31Hz, 1 H), 7.38-7.39(d, J=8.31Hz, 2H), 7.42-7.44(d, J=7.82Hz, 1H), 7.47-7.48(d, J=8.31Hz, 2H), 8.34(brs, 1H) (S)-4-Bromo-N-(1-(2-decanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide 1 H-NMR (500MHz, CDCl3) δ0.87-0.89(t, J=6.35Hz, 3H), 1.28(s, 12H), 1.50-1.54(m, 2H), 2.28-2.39(m, 2H) ), 3.13-3.23(dd, J=14.67, 7.33Hz, 1H), 3.23-3.27(dd, J=14.67, 5.38Hz, 1H), 4.36-4.39(t, J=6.84Hz, 1 H), 7.02(s, 1H), 7.06-7.09(t, J=7.82Hz, 1H), 7.19-7.22(t, J=7.33Hz, 1H), 7.33-7.34(d, J=8.31Hz, 1H) , 7.39-7.40(d, J=8.31Hz, 2H), 7.42-7.44(d, J=7.82Hz, 1H), 7.47-7.48(d, J=8.31Hz, 2H), 8.33(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-pentylpropanamide 1 H-NMR (500MHz, CDCl3) δ2.60-2.73(m, 2H), 2.93-2.98(dd, J=14.18, 7.82Hz, 1H), 3.17-3.21(dd, J=14. 67, 5.38Hz, 1H), 3.33-3.40(dq, J=13.69, 6.84x3Hz, 1H), 3.43-3.49(dq, J=13.20, 6.84x2, 6.35Hz, 1H) , 3.83-3.87(q, J=6.35x2, 6.84Hz, 1H), 5.26-5.27(d, J=6.35Hz, 1H), 6.36-6.38(t, J=5.38Hz, 1H), 6.8 2(s, 1H), 7.00-7.03(t, J=7.33Hz, 1H), 7.06-7.08(d, J=7.82Hz, 2H), 7.19-7.31(m, 10H), 8.16(brs, 1H) N-((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide 1 H-NMR (500MHz, CDCl3) δ1.66-1.75(m, 6H), 1.89(s, 6H), 2.03(s, 3H), 3.03-3.07(dd, J=14.67, 9.29Hz, 1H), 3.26-3.30(dd, J=15.16, 4.89Hz , 1H), 4.27(brs, 1H), 6.54(brs, 1H), 6.96-7.01(m, 2H), 7.13-7.18(m, 3H), 7.24-7.32(m, 4H), 8.32(brs, 1H), 8.49(brs, 1H), 9.66(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-N-(4-fluoropentyl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, CDCl3) δ2.59-2.71(m, 2H), 2.92-3.00(m, 1H), 3.18-3.22(dd, J=14.67, 5.86Hz, 1H), 3.31-3.37(m, 1H), 3.43- 3.49(m, 1H), 3.83-3.87(m, 1H), 5.19-5.22(m, 1H), 6.41-6.43(m, 1H), 6.86-7.04(m, 5H), 7.20-7.35(m, 7H), 8.17-7.20(m, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-methoxypentyl)propanamide 1H-NMR (500MHz, CDCl3) δ2.55-2.67(m, 2H), 2.95-3.00(m, 1H), 3.17-3.21 (m, 1H), 3.32-3.35(m, 1H), 3.41-3.45(m, 1H), 3.77-3.78(d, J=4.40Hz, 3H ), 3.86(m, 1H), 5.21-5.23(t, J=4.40Hz, 1H), 6.34-6.35(d, J=4.40Hz, 1H ), 6.80-6.82(m, 3H), 6.98-7.05(m, 3H), 7.20-7.33(m, 7H), 8.17(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(3-phenylpropyl)propanamide 1 H-NMR (500MHz, CDCl3) δ1.69-1.74 (m, 2H), 2.53-2.56 (t, 6.84Hz, 2H), 2.95-2.99 (dd, J=14.67, 6.84Hz, 1H), 3.13-3.19(m, 1H), 3.22-3.26(dd, J=13.20, 5.86Hz, 2H ), 3.83-3.86(m, 1H), 5.20-5.21(d, J=3.91Hz, 1H), 6.37(brs, 1H), 6.90(s, 1H), 7 .00-7.03(m, 1H), 7.11-7.12(d, J=7.33Hz, 2H), 7.17-7.31(m, 10H), 8.15(brs, 1H) (S)-N-((3R,5R,7R)-adamantan-1-yl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide 1H-NMR (500MHz, CDCl3) δ1.58-1.64(m, 6H), 1.74-1.80(m, 6H), 2.01(s, 3H), 3.05-3.09(d d, J=14.67, 7.33Hz, 1H), 3.15-3.20(dd, J=14.67, 6.84Hz, 1H), 3.77-3.81(q, J=7.33, 6. 84, 6.35Hz, 1H), 5.35-5.36(d, J=6.35Hz, 1H), 5.65(s, 1H), 6.96(d, J=1.95Hz, 1H), 7.04 -7.07(t, J=7.82Hz, 1H), 7.20-7.23(t, J=7.82Hz, 1H), 7.33-7.39(m, 6H), 8.21(brs, 1H) (S)-N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide 1 H-NMR (500MHz, CDCl3) δ1.77-1.80(t, J=8.31Hz, 1H), 2.34-2.41(m, 2H), 2.62-2.66(m, 1H), 2.78-2.81(m, 1H), 2.92 -2.97(m, 1H), 3.10-3.16(m, 2H), 3.19-3.23(m, 1H), 3.38-3.42(m, 1H), 3.76(s, 3H), 4.48-4.53(m, 1H), 6.02-6.04( d, J=9.78Hz, 1H), 6.68-6.66(m, 2H), 6.77-6.80(m, 2H), 7.04(d, J=2.44Hz, 1H), 7.11-7.14(t, J=7.82Hz, 1H), 7.17- 7.20(t, J=7.33Hz, 1H), 7.30-7.31(d, J=8.31Hz, 1H), 7.50-7.54(m, 3H), 7.62-7.64(d, J=8.31Hz, 2H), 8.11(brs, 1H) (S)-N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide 1H-NMR (500MHz, CDCl3) δ1.65-1.69(m, 1H), 2.21-2.24(m, 1H), 2.28-2.37(m, 4H), 2.53-2.56(m, 1H), 2.66-2.69(m, 1H), 2.81-2.84(m, 1H), 3.04- 3.15(m, 2H), 3.21-3.25(dd, J=13.69, 4.89Hz, 1H), 3.32-3.35(m, 1H), 3 .75(s, 3H), 4.45-4.50(td, J=5.38x2, 4.40Hz, 1H), 5.91-5.93(d, J=9.78 Hz, 1H), 6.59-6.61(d, J=9.29Hz, 2H), 6.77-6.79(d, J=9.29Hz, 2H), 7.0 5-7.06(d, J=2.44Hz, 1H), 7.10-7.13(t, J=7.82Hz, 1H), 7.16-7.19(t, J= 7.33Hz, 1H), 7.20-7.22(d, J=8.31Hz, 2H), 7.29-7.31(d, J=7.82Hz, 1H), 7.51-7.53(d, J=7.82Hz, 1H), 7.68-7.70(d, J=8.31Hz, 2H, 8.14(brs, 1H) (S)-N-((3R,5R,7R)-adamantan-1-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, CDCl3) δ1.57-1.64(m, 6H), 1.74-1.80(m, 6H), 2.00(brs, 3H), 2.34(s, 3H), 3.04-3 .08(m, 1H), 3.12-3.16(m, 1H), 3.78-3.82(q, J=6.84, 6.35x2Hz, 1H), 5.13-5.14(d, J=6.35Hz, 1H) , 5.75(s, 1H), 6.94-6.95(d, J=1.46Hz, 1H), 7.01-7.04(t, J=7.33Hz, 1H), 7.08-7.09(d, J=7.82Hz , 2H), 7.15-7.19(m, 1H), 7.32-7.36(t, J=8.80Hz, 2H), 7.48-7.50(d, J=8.31Hz, 2H), 8.27(brs, 1H) (S)-3-(1H-indol-3-yl)-N-(4-methoxypentyl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500MHz, CDCl3) δ2.33(s, 3H), 2.50-2.63(m, 2H), 3.01-3.10(m, 2H), 3.30-3.40(m, 2H), 3.77 (s, 3H), 3.85-3.89(q, J=6.35Hz, 1H), 5.03-5.04(d, J=5.86Hz, 1H), 6.36-6.38(t, 5.38Hz, 1H), 6.7 7-6.81(m, 3H), 6.93-6.95(d, J=8.80Hz, 2H), 6.98-7.01(t, J=7.33Hz, 1H), 7.04-7.06(d, J=7.82Hz , 2H), 7.15-7.18(t, J=7.82Hz, 1H), 7.26-7.31(m, 2H), 7.43-7.45(d, J=8.31Hz, 2H), 8.22(brs, 1H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(3-phenylpropyl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ1.40-1.46(m, 2H), 2.23(s, 3H), 2.34-2.37(t, J=7.33Hz, 2H), 2.75-2.8 3(m, 3H), 2.94-2.99(dd, J=14.18, 6.84Hz, 1H), 3.89-3.92(t, J=6.84Hz, 1H), 6.90-6.93(t, J=7.3 3Hz, 1H), 7.01-7.04(t, J=7.33Hz, 1H), 7.07-7.17(m, 6H), 7.24-7.28(m, 3H), 7.34-7.36(d, J=7.8 2Hz, 1H), 7.48-7.49(d, J=7.82Hz, 2H), 7.85-7.87(t, J=5.38Hz, 1H), 7.93(brs, 1H), 10.77(s, 1H) (S)-N-(4-fluoropentyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (500MHz, CD3OD) δ2.28(s, 3H), 2.49-2.54(m, 2H), 2.80-2.84(dd, J=14.18, 7.82Hz, 1H), 3.07-3.14(m, 2H), 3.23-3.27(m, 1H), 3. 86-3.89(t, J=7.82Hz, 1H), 6.92-7.06(m, 9H), 7.26-7.27(d, J=7.82Hz, 1H), 7.31-7.33(d, J=7.82Hz, 1H), 7.40-7.42(d, J=7.82Hz, 2H) (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.15(s, 3H), 2.85-2.90(dd, J=14.67, 7.82Hz, 1H), 3.07-3.11(dd, J =14.67, 6.84Hz, 1H), 4.28-4.31(t, J=7.33Hz, 1H), 6.89-6.92(t, J=7.33Hz, 1H), 7.01-7.06(m , 4H), 7.26-7.28(d, J=8.31Hz, 1H), 7.40-7.42(d, J=7.82Hz, 1H), 7.45-7.47(d, J=8.31Hz, 2H) , 7.78-7.80(m, 3H), 8.06-8.08(d, J=8.31Hz, 2H), 8.27(brs, 1H), 10.78(s, 1H), 12.39(brs, 1H) (S)-N-(2-(1H-indol-3-yl)ethyl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide 1H-NMR (500MHz, CD3OD) δ2.72-2.84(m, 3H), 3.14-3.18(dd, J=14.67, 5.38Hz, 1H ), 3.27-3.30(m, 1H), 3.38-3.42(m, 1H), 3.92-3.95(dd, 9.29, 5.38Hz, 1H), 6.9 3-6.96(m, 2H), 6.99-7.03(m, 2H), 7.07-7.11(m, 2H), 7.22-7.24(m, 2H), 7.27- 7.29(m, 3H), 7.32-7.36(dd, J=7.82, 4.40Hz, 2H), 7.52-7.53(d, J=7.82Hz, 1H) (S)-N-(3-(1H-indol-3-yl)-1-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-1-oxopropan-2-yl)-4-methylbenzamide 1 H-NMR (500MHz, DMSO-d6) δ2.33(s, 3H), 3.23-3.34(m, 2H), 3.78(s, 3H), 4.95-4 .99(m, 1H), 6.97-7.00(m, 3H), 7.04-7.07(t, J=7.82Hz, 1H), 7.24-7.26(d, J=7. 82Hz, 2H), 7.30-7.32(m, 2H), 7.45(s, 1H), 7.73-7.75(d, J=7.82Hz, 2H), 7.83-7 .84(d, J=8.80Hz, 3H), 8.62-8.63(d, J=7.82Hz, 1H), 10.84(s, 1H), 12.64(s, 1H) (S)-2-(4-chlorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.86-2.91 (dd, J=14.18, 8.80Hz, 1H), 3.08-3.12 (dd, J=14.67, 6.35Hz, 1H), 3. 78(s, 3H), 4.33(brs, 1H), 6.90-6.93(t, J=7.33Hz, 1H), 6.97-6.99(d, J=8.80Hz, 2H), 7.02-7.05(t, J=7.3 3Hz, 1H), 7.08(d, J=1.95Hz, 1H), 7.22-7.24(d, J=8.80Hz, 2H), 7.26-7.27(d, J=8.31Hz, 1H), 7.43(s, 1H) , 7.46-7.48(d, J=8.80Hz, 3H), 7.79-7.81(d, J=8.80Hz, 2H), 8.50(brs, 1H), 10.78(s, 1H), 12.44(brs, 1H) (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-(trifluoromethyl)phenylsulfonamido)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.88-2.93(dd, J=14.67, 9.29Hz, 1H), 3.09-3.13(dd, J=14.18, 5. 18Hz, 1H), 3.78(s, 3H), 4.37(brs, 1H), 6.88-6.91(t, J=7.33Hz, 1H), 6.97-7.02(m, 3H), 7.10 (d, J=1.95Hz, 1H), 7.22-7.24(d, J=8.31Hz, 1H), 7.42(s, 1H), 7.48-7.53(m, 3H), 7.65-7.67( d, J=7.82Hz, 2H), 7.79-7.80(d, J=8.31Hz, 2H), 8.70(brs, 1H), 10.77(s, 1H), 12.46(brs, 1H) (S)-2-(4-fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (500MHz, CD3OD) δ2.87-2.92(dd, J=14.67, 8.80, Hz, 1H), 3.08-3.12(dd, J=14.18, 6.35Hz, 1H), 3.76(s, 3H), 4.28-4.31(dd, J=8.31, 6.84Hz, 1H), 6.89-6 .92(m, 1H), 6.96-7.06(m, 4H), 7.08(s, 1H), 7.26-7.28(m, 1H), 7.39(s, 1H), 7.4 6-7.47(d, J=7.82Hz, 1H), 7.54-7.58(m, 2H), 7.78-7.81(m, 2H), 10.82(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-N-((1r,3R,5S,7S)-3,5-dimethyladamantan-1-yl)-3-(1H-indol-3-yl)propanamide 1 H-NMR (500MHz, CDCl3) δ0.80(s, 6H), 1.08(s, 2H), 1.22-1.43(m, 8H), 1.59(s, 2H), 2.07(s, 1H), 3.0 3-3.07(dd, J=14.67, 7.33Hz, 1H), 3.16-3.20(dd, J=14.67, 6.84Hz, 1H), 3.77-3.80(m, 1H), 5.36-5 .37(d, J=6.35Hz, 1H), 5.70(s, 1H), 6.97(s, 1H), 7.03-7.06(t, J=7.33Hz, 1H), 7.20-7.23(t, J=7.3 3Hz, 1H), 7.32-7.38(m, 4H), 7.63-7.64(d, J=8.80Hz, 1H), 7.77-7.79(d, J=8.31Hz, 1H), 8.20(s, 1H) (S)-2-(4-cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.85-2.90(dd, J=14.67, 9.78Hz, 1H), 3.05-3.09(dd, J=14.1 8, 5.38Hz, 1H), 3.78(s, 3H), 4.34(brs, 1H), 6.89-6.92(t, J=7.82Hz, 1H), 6.98-7.04(m, 3H), 7.07-7.08(d, J=1.95Hz, 1H), 7.22-7.23(d, J=8.31Hz, 1H), 7.46-7.52(m, 6H), 7.82 -7.83(d, J=8.80Hz, 2H), 8.74(brs, 1H), 10.72-10.72(d, J=1.46Hz, 1H), 12.58(brs, 1H) (S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate 1 H-NMR (500MHz, CDCl3) δ3.36-3.43(m, 2H), 5.03-5.10(m, 2H), 5.15-5.18(dt, J=7.82, 5.38x2Hz, 1H), 6.69-6.70(d, J=2.44Hz, 1H), 6.76-6.78(d, J=7.82Hz, 1H), 7.01-7.04 (t, J=7.33Hz, 1H), 7.07-7.08(d, J=8.31Hz, 2H), 7.10-7.13(t, J=7.33Hz, 1H), 7.21-7 .31(m, 6H), 7.50-7.51(d, J=7.82Hz, 1H), 7.53-7.54(d, J=8.31Hz, 2H), 8.64(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(5-hydroxy-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.79-2.83(dd, J=14.18, 8.31Hz, 1H), 2.99-3.03(dd, J=14.18, 6.84Hz, 1H), 3.77(s, 3H), 4.31-4.34(q, J=8.31, 7.82, 7.33Hz, 1H), 6.58-6.60(dd, J=8.80, 2.44Hz, 1H), 6. 86(d, J=1.95Hz, 1H), 6.97-6.99(m, 3H), 7.06-7.07(d, J=8.80Hz, 1H), 7.40-7.46(m, 4H), 7.77-7.8 4(m, 2H), 8.46-8.48(d, J=8.31Hz, 1H), 8.61(brs, 1H), 10.47-10.48(d, J=1.95Hz, 1H), 12.4(s, 1H) (S)-2-(4-bromophenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-3-(5-methyl-1H-indol-3-yl)propanamide 1 H-NMR (500MHz, DMSO-d6) δ2.33 (s, 3H), 2.82-2.86 (dd, J=14.18, 8.31Hz, 1H) , 3.04-3.09(dd, J=14.67, 6.84Hz, 1H), 3.77(s, 3H), 4.29(brs, 1H), 6.84-6. 86(d, J=8.31Hz, 1H), 6.97-7.02(m, 3H), 7.14-7.16(m, 2H), 7.41-7.45(m, 5H ), 7.79-7.81(d, J=8.31Hz, 2H), 8.47(brs, 1H), 10.64(s, 1H), 12.40(brs, 1H) (S)-2-(4-bromophenylsulfonamido)-3-(5-fluoro-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.97-3.02(dd, J=14.18, 8.80Hz, 1H), 3.17-3.22(dd, J=14.18, 5.86Hz, 1H), 3.8 1(s, 3H), 4.24-4.27(dd, J=8.80, 6.35Hz, 1H), 4.62(s, 1H), 6.81-6.85(td, J=9.29x2, 2.44Hz, 1H), 6.92-6 .94(d, J=8.80Hz, 2H), 7.08(s, 1H), 7.12-7.14(dd, J=10.27, 1.95Hz, 1H), 7.17(s, 1H), 7.21-7.22(dd, J=8 .80, 4.40Hz, 1H), 7.27-7.29(d, J=8.31Hz, 2H), 7.41-7.43(d, J=8.31Hz, 2H), 7.77-7.79(d, J=8.31Hz, 2H) (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)ethyl)benzoic acid 1 H-NMR (500MHz, DMSO-d6) δ2.28(s, 3H), 2.54-2.64(m, 2H), 2.80-2.85(dd, J=14.18, 7.82Hz, 1H), 3.09-3.20(m, 2H) ), 3.26-3.30(dd, J=13.20, 6.35Hz, 1H), 3.86-3.89(dd, J=7.82, 6.35Hz, 1H), 6.90-6.93(t, J=7.82Hz, 1H), 6.95(s , 1H), 7.00-7.02(d, J=8.31Hz, 2H), 7.04-7.07(t, J=6.84Hz, 1H), 7.14-7.15(d, J=8.31Hz, 2H), 7.26-7.27(d, J=7 .82Hz, 1H), 7.31-7.32(d, J=7.82Hz, 1H), 7.40-7.41(d, J=8.31Hz, 2H), 7.90-7.91(d, J=7.82Hz, 3H), 10.22(s, 1H) (S)-N-(4-bromopentyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.27(s, 3H), 2.36-2.43(m, 2H), 2.69-2.73(dd, J=14.18, 7.82Hz, 1H), 2.88-2.98(m, 2 H), 3.03-3.08(dt, J=13.20, 6.84, 6.35Hz, 1H), 3.82-3.85(t, J=6.84Hz, 1H), 6.89-6.92(t, J=7.33Hz, 1H), 6.97 -6.99(d, 8.31Hz, 2H), 7.01-7.04(t, J=7.33Hz, 2H), 7.12-7.14(d, J=8.31Hz, 2H), 7.28-7.32(dd, J=11.24, 8.31 Hz, 2H), 7.37-7.39(d, J=7.33Hz, 2H), 7.44-7.46(d, J=7.82Hz, 2H), 7.91-7.93(t, J=5.38Hz, 2H), 10.75(brs, 1H) (S)-N-(2-(1H-indol-3-yl)ethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1 H-NMR (500Mz, CD3OD) δ2.24(s, 3H), 2.64-2.76(m, 2H), 2.82-2.86(dd, J=14.67, 8.31Hz , 1H), 3.11-3.15(dd, J=14.67, 5.86Hz, 1H), 3.20-3.26(m, 1H), 3.30-3.36(m, 1H), 3.89- 3.91(dd, J=8.31, 6.35Hz, 1H), 6.91-7.01(m, 6H), 7.04-7.10(m, 2H), 7.25-7.27(d, J=7. 82Hz, 1H), 7.32-7.35(m, 2H), 7.36-7.38(d, J=8.31Hz, 2H), 7.48-7.49(d, J=7.82Hz, 1H) (S)-3-(1H-indol-3-yl)-N-(4-methylpentyl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (500MHz, CD3OD) δ2.27-2.27(d, J=4.89Hz, 6H), 2.43-2.54(m, 2H), 2.80-2.85(dd, J=14.18, 8.13Hz, 1H), 3.07-3.14(m, 2H), 3.21-3.26(m , 1H), 3.86-3.89(t, J=6.84Hz, 1H), 6.91-7.07(m, 9H), 7.25-7.27(d, J= 7.82Hz, 1H), 7.32-7.33(d, J=7.82Hz, 1H), 7.40-7.41(d, J=7.82Hz, 2H) Ethyl 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoate 1 H-NMR (500MHz, CD3OD) δ1.07-1.10(t, J=7.33Hz, 3H), 2.18(s, 3H), 2.80-2.85(dd, J=14.67, 8 .80Hz, 1H), 3.06-3.18(m, 3H), 3.97-4.05(m, 3H), 4.53-4.55(t, J=6.84Hz, 1H), 6.82-6.84(d, J=7.82Hz, 2H), 6.90-6.94(m, 1H), 6.96(s, 1H), 7.00-7.06(m, 3H), 7.10-7.13(td, J=7.82,7.3 3Hz, 1H), 7.24-7.26(d, J=7.82Hz, 1H), 7.29-7.30(d, J=8.31Hz, 2H), 7.34-7.36(dt, J=8.31x2 Hz, 2H), 7.45-7.46(d, J=7.82Hz, 1H) (S)-N-(4-chloropentyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (500MHz, CD3OD) δ2.29(s, 3H), 2.46-2.57(m, 2H), 2.80-2.84(dd, J=14.1 8, 7.82Hz, 1H), 3.07-3.14(m, 2H), 3.24-3.29(m, 1H), 3.86-3.89(t, J=6.35Hz, 1 H), 6.91-6.96(m, 2H), 7.02-7.08(m, 5H), 7.19-7.21(d, J=8.31Hz, 2H), 7.26-7. 28(d, J=7.82Hz, 1H), 7.31-7.33(d, J=7.82Hz, 1H), 7.41-7.42(d, J=7.82Hz, 2H) 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoic acid 1 H-NMR (500MHz, CD3OD) δ2.18(s, 3H), 2.57-2.62(dd, J=14.67, 10.27, Hz, 1H), 3.12-3.21(dd, J=14.67, 3. 42Hz, 1H), 3.21-3.25(dd, J=14.67, 6.35Hz, 1H), 3.37-3.41(dd, J=14.67, 4.89Hz, 1H), 3.87-3.89(dd, J= 9.78, 3.91Hz, 1H), 4.51-4.53(t, J=5.86Hz, 1H), 6.72-6.74(d, J=8.31Hz, 2H), 6.84(s, 1H), 6.86-6.89(t, J=7.82Hz, 1H), 6.97-7.00(t, J=7.8 2Hz, 1H), 7.02-7.09(m, 2H), 7.13-7.15(m, 3H), 7.20-7.21(d, J=7.82Hz, 1H), 7.29-7.32(dd, J=7.33, 6.84Hz, 2H), 7.59-7.61(d, J=7.82Hz, 1H) (S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate 1H-NMR (500MHz, DMSO-d6) δ2.16(s, 3H), 2.49-2.50(dd, J=14.18, 7.82, 6.35Hz, 1H), 3.07-3 .11(dd, J=14.18, 7.33, 6.84Hz, 1H), 3.85(s, 3H), 4.30(brs, 1H), 6.89-6.92(t, J=7.33Hz, 1 H), 7.01-7.07(m, 4H), 7.26-7.28(d, J=7.82Hz, 1H), 7.41-7.42(d, J=7.82Hz, 1H), 7.45-7.4 7(d, J=8.31Hz, 2H), 7.80(s, 1H), 8.01(s, 4H), 8.27(brs, 1H), 10.79(s, 1H), 12.41(brs, 1H) (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoic acid 1 H-NMR (500MHz, DMSO-d6) δ2.18(s, 3H), 2.87-2.91(dd, J=14.18, 7.82Hz, 1H), 3.09-3.13(dd, J=14 .18, 6.84Hz, 1H), 4.31-4.36(q, J=7.82x3Hz, 1H), 6.91-6.94(t, J=7.33Hz, 1H), 7.03-7.09(m, 4H) , 7.28-7.30(d, J=7.82Hz, 1H), 7.43-7.44(d, J=7.82Hz, 1H), 7.47-7.49(d, J=7.82Hz, 2H), 7.80(s , 1H), 7.99-8.03(m, 4H), 8.28-8.30(d, J=8.80Hz, 1H), 10.81(s, 1H), 12.43(s, 1H), 12.98(brs, 1H) (S)-3-(benzo[d]oxazol-2-ylamino)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide 1H-NMR (500MHz, DMSO-d6) δ2.13(s, 3H), 3.51-3.55(m, 2H), 3.79(s, 3H), 4.35-4.36(d, J=5.38Hz, 1H), 6.98-7.01(m, 3H), 7.11-7.15(m, 3H), 7.22-7.24(d, J=7.82Hz, 1H), 7.3 0-7.32(d, J=7.82Hz, 1H), 7.44(s, 1H), 7.65-7.66(d, J=8.31Hz, 2H), 7.80-7.82(d, J=8 .31Hz, 2H), 7.99-8.01(t, J=6.35Hz, 1H), 8.20-8.21(d, J=5.86Hz, 1H), 12.33(brs, 1H) (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)benzamide 1 H-NMR (500MHz, CD3OD) δ2.20(s, 3H), 3.63-3.67(m, 1H), 3.73-3.75(m, 1H) , 3.88(s, 3H), 4.33-4.35(t, J=6.35Hz, 1H), 6.99-7.01(d, J=8.80Hz, 2H), 7.17-7.18(d, J=7.82Hz, 2H), 7.24(s, 1H), 7.47-7.50(m, 2H), 7.57-7.60( m, 1H), 7.74-7.78(dd, J=14.18, 7.82Hz, 4H), 7.85-7.86(d, J=8.31Hz, 2H) (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)nicotinamide 1H-NMR (500MHz, DMSO-d6) δ2.14(s, 3H), 3.48-3.53(dt, J=13.20, 6.84, 6.35Hz, 1H), 3.56-3.63(m, 1H), 3.78(s , 3H), 4.23-4.26(t, J=6.84Hz, 1H), 6.97-6.99(d, J=8.80Hz, 2H), 7.14-7.16(d, J=8.31Hz, 2H), 7.42(s, 1H), 7 .45-7.48(dd, J=7.82, 4.89, 2.93Hz, 1H), 7.64-7.66(d, J=8.31Hz, 2H), 7.79-7.80(d, J=8.80Hz, 2H), 8.01-8. 03(dt, J=7.82, 1.95x2Hz, 1H), 8.11(brs, 1H), 8.65-8.68(m, 2H), 8.84-8.85(d, J=1.46Hz, 1H), 12.28(brs, 1H) (S)-N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)pyrimidine e-5-carboxamide 1 H-NMR (500MHz, DMSO-d6) δ2.16(s, 3H), 3.49-3.53(dt, J=13.69, 6.84x2Hz, 1H), 3.57-3.63(dt, J =13.20, 6.35x2Hz, 1H), 3.79(s, 3H), 4.23-4.26(m, 1H), 6.98-7.00(d, J=8.80Hz, 2H), 7.17-7.19 (d, J=8.31Hz, 2H), 7.45(s, 1H), 7.65-7.67(d, J=8.31Hz, 2H), 7.79-7.81(d, J=8.80Hz, 2H), 8.18 -8.19(d, J=7.82Hz, 1H), 8.87-8.89(t, J=5.86Hz, 1H), 9.00(s, 2H), 9.31(s, 1H), 12.31(brs, 1H)

[0055] Example 2: DX2-nanoluciferase activity (40 μM) and cell viability (% inhibition) After cloning DX2 into a plasmid expressing nanoluciferase, the corresponding plasmid was transformed into A549 cells. The transformed cells were plated in a 96-well plate at 1X10 per well. 4 The cells were seeded one by one and allowed to stabilize for 12 hours. Compounds were treated for 4 hours, after which the expression changes of DX2 were observed through luciferase assay. A549 cells were treated with various concentrations of compounds, and cell viability was measured by the MTT method 72 hours later. The results in this regard are shown in Table 1 above.

[0056] Example 3: Evaluation of AIMP2-DX2 and AIMP2 inhibitory activity (nanoluciferase assay) Among the compounds in Table 1 that showed excellent effects, compound 63 was selected and the following experiment was carried out. To measure the IC50 of Compound 63, A549 cells expressing nanoluciferase-DX2 or AIMP2 were treated with Compound 63 at different concentrations for 4 hours, and then fluorescence was measured. The results in this regard are shown in FIG. As shown in FIG. 1, the inhibition rates of compound 63 against AIMP2-DX2 and -AIMP2 were confirmed to show a selectivity of 100 times or more over AIMP2-DX2 (DX2 IC50 = 0.92 μM and AIMP2 IC50 > 100 μM).

[0057] Example 4: Mechanistic studies of AIMP2-DX2 inhibition According to previous reports, AIMP2-DX2 is stabilized by binding with HSP70. Therefore, the present inventors confirmed whether compound 63, which shows the most excellent AIMP2-DX2 inhibitory activity, can inhibit the binding of AIMP2-DX2 to HSP70. Specifically, an in vitro pull-down assay was performed using purified AIMP2-DX2 and HSP70 proteins in the presence of Compound 63. The results in this regard are shown in FIG. As shown in FIG. 2, it was confirmed that Compound 63 inhibited the binding between AIMP2-DX2 and HSP70 in a concentration-dependent manner.

[0058] Example 5: Evaluation of in vivo anticancer effects Next, the anticancer effect of compound 63 was evaluated in a mouse model implanted with H460 cells. Specifically, Compound 63 was intraperitoneally administered at 50 mg / kg to mice transplanted with H460 cells once every two days for a total of 15 days. The results in this regard are shown in Figures 3a to 3d. As shown in Figures 3a to 3d, it was confirmed that compound 63 significantly inhibited tumor growth, and there was no change in the body weight of the animals during the administration period.

[0059] Example 6: In vivo cancer growth inhibition effects of Compound 55 and Compound 89 Furthermore, compounds 55 and 88 were selected from Table 1 and subjected to an experiment on their in vivo cancer growth inhibitory effect. H460 cells (2X10 7 ) was inoculated subcutaneously into 7-week-old BALB / cAnCr female rats, and then compound 55 or compound 89 (50 mg / kg) and taxol (10 mg / kg) were administered intraperitoneally once every two days. The drugs were administered for 16 days, and the tumor size and animal weight at the time of administration were measured. After 16 days, the animals were sacrificed, and the size and weight of the removed tumor were measured. The results in this regard are shown in FIG. At the concentration administered, compound 55 exhibited a tumor growth inhibitory effect of approximately 50% during the treatment period, and since it was confirmed that there was no change in the body weight of the animals during the treatment period, it is determined that the compound has no side effects. [Industrial Applicability]

[0060] The compound represented by Chemical Formula 1 according to the present invention has an excellent effect of inhibiting the expression of AIMP2-DX2, and can be very usefully used in the development of therapeutic agents for various diseases induced by AIMP2-DX2, especially cancer.

Claims

1. A compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] 【Chemistry 1】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemistry 2】 Or, 【Chemistry 3】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 12 below. 【Chemistry 4】 【Chemistry 5】

2. 2. The compound according to claim 1, which inhibits the expression of AIMP2-DX2, or a pharma- ceutically acceptable salt thereof.

3. A pharmaceutical composition for preventing or treating cancer, comprising as an active ingredient a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] 【Chemistry 6】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemistry 7】 Or, 【Chemistry 8】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemistry 9】 【Chemistry 10】

4. The pharmaceutical composition of claim 3, wherein the cancer is selected from the group consisting of leukemia, brain cancer, kidney cancer, stomach cancer, skin cancer, bladder cancer, breast cancer, uterine cancer, melanoma, thyroid cancer, head and neck cancer, lymphoma, gallbladder cancer, esophageal cancer, lung cancer, colon cancer, prostate cancer, ovarian cancer, liver cancer, colorectal cancer, peritoneal cancer, peritoneal metastasis cancer and pancreatic cancer.

5. A pharmaceutical composition for preventing or treating an inflammatory disease, comprising as an active ingredient a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] 【Chemistry 11】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemistry 12】 Or, 【Chemistry 13】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemistry 14】 【Chemistry 15】

6. The inflammatory diseases include inflammatory skin diseases, Crohn's disease, ulcerative colitis, peritonitis, osteomyelitis, cellulitis, meningitis, encephalitis, pancreatitis, trauma-induced shock, bronchial asthma, allergic rhinitis, cystic fibrosis, stroke, acute bronchitis, chronic bronchitis, acute bronchiolitis, chronic bronchiolitis, osteoarthritis, gout, spondyloarthropathy, ankylosing spondylitis, Reiter's syndrome, psoriatic arthropathy, enteropathic spondylitis, juvenile arthropathy, juvenile ankylosing spondylitis, reactive arthropathy, infectious arthropathy, and the like. Arthritis, post-infectious arthritis, gonococcal arthritis, tuberculous arthritis, viral arthritis, fungal arthritis, syphilitic arthritis, Lyme disease, arthritis associated with the "vasculitis syndrome," polyarteritis nodosa, hypersensitivity vasculitis, Lou Gehrig's granulomatosis, polymyalgia rheumatica, articular cell arteritis, calcium crystal deposition arthropathy, pseudogout, non-rheumatoid arthritis, mucositis, tenosynovitis, epicondylitis (tennis elbow), neuropathic joint disease (charcoal arthritis, sclerosing ...

6. The pharmaceutical composition according to claim 5, characterized in that the inflammatory bowel disease is selected from the group consisting of hemoglobinopathy, hemorrhagic arthropathy, hemarthrosic, Henoch-Schönlein purpura, hypertrophic osteoarthropathy, multicentric reticulohistiocytosis, sarcoilosis, hemochromatosis, sickle cell disease and other hemochromatosis, hyperlipoproteinemia, hypogammaglobulinemia, familial Mediterranean fever, Behat's disease, systemic lupus erythematosus, relapsing fever, psoriasis, multiple sclerosis, sepsis, septic shock, multiple organ dysfunction syndrome, acute respiratory distress syndrome, chronic obstructive pulmonary disease, rheumatoid arthritis, acute lung injury and broncho-pulmonary dysplasia.

7. Use of a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof for the manufacture of a preparation for the prophylaxis or treatment of cancer. [Chemical formula 1] 【Chemistry 16】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemistry 17】 Or, 【Chemistry 18】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemistry 19】 【Chemistry 20】

8. A method for treating cancer, comprising administering to an individual, other than a human, in need thereof an effective amount of a composition containing, as an active ingredient, a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] 【Chemistry 21】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemical 22】 Or, 【Chemistry 23】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemistry 24】 【Chemistry 25】

9. A method for treating an inflammatory disease, comprising administering to an individual, other than a human, in need thereof an effective amount of a composition containing, as an active ingredient, a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof: [Chemical formula 1] 【Chemistry 26】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemical 27】 Or, 【Chemistry 28】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemical Formula 29】 【Chemistry 30】

10. Use of a compound represented by the following chemical formula 1 or a pharma- ceutically acceptable salt thereof for producing a preparation for treating an inflammatory disease. [Chemical formula 1] 【Chemistry 31】 In the above formula 1, R 1 is a C1-C5 linear or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1-C5 alkylthio; or an indolylmethyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1-C5 alkyl, hydroxy, hydroxycarbonyl, and formyl; R 2 is unsubstituted or substituted benzenesulfonyl with one or more substituents selected from the group consisting of C1-C5 linear or branched alkyl, nitro group, amine group, halo, -CF 3 , C1-C5 alkylcarbonylamino, -COOH, C1-C5 alkoxy, phenyl, -OCH 2 Ph, hydroxy, -COOCH 2 Ph, C1-C5 alkyloxycarbonyl, -CONHCH 3 , and nitrile; R3 is 【Chemistry 32】 Or, 【Chemical 33】 and The combination of R 1 , R 2 , and R 3 is selected from the group consisting of combinations 1 to 13 below. 【Chemical 34】 【Chemistry 35】

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