168 results about "Beta-Carboline" patented technology

A composition includes a substituted dihydro- or tetrahydro-beta-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-beta-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

A soft capsule containing a solution or suspension of a PDE5 inhibitor, and use of the capsule in treating sexual dysfunction.

The present invention relates to a harmine derivative compound and the application. The compound is produced through the structural modification of the 1st, 2nd, 3rd, 7th and 9th pint of the parent nuclear of the beta-carboline of the harmine; thus the novel harmine derivative compound is synthesized with the enhanced anti-tumor activity and no toxicity of the nervous system. Through the screening research of the vitro and vivo anti-tumor model, the harmine derivative compound is found to have the significant anti-tumor activity (the tumor-inhibition rate of the tumor-bearing mice model reaches as high as 63.5 percent), have no neurotoxicity, and have the prospects of clinical application. The preparation method of the compound is simple; the collection rate is high; and the compound is used for the drugs of treating various tumor diseases.

Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure:where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.

The invention discloses 16 pseudopeptides represented by a general formula I (wherein in the general formula I, AA is equal to L-Ala, Gly, L-Leu, L-Ile, L-Val, L-Phe, L-Asp, L-Glu, L-Ser,L-Thr, L-Asn, L-Trp, L-Tyr, L-Met, L-Pro and Lys residue and further discloses a preparation method and application thereof. The pseudopeptides show excellent in-vitro and in-vivo anti-tumor effects in a cell model and an S180 tumor-bearing mouse model and an excellent anti-inflammatory effect in a mouse ear swelling model.

The invention discloses a di-beta-carboline alkali compound and a preparation method, a medicinal composition and application thereof. The di-beta-carboline alkali compound and pharmaceutical salt thereof are shown as a general formula I. The di-beta-carboline alkali compound is prepared by condensing a beta-carboline intermediate and dihalogenated alkane. The medicinal composition comprises an effective dose of di-beta-carboline alkali compound shown as the formula I and a pharmacodynamically acceptable carrier. The invention also discloses application of the di-beta-carboline alkali compound to preparation of medicines for resisting tumors such as melanoma, gastric cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermal carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostatic cancer and colon cancer.

A composition includes a substituted dihydro- or tetrahydro-beta-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-beta-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

The invention relates to beta-carboline alkali derivative compounds and application thereof. Novel beta-carboline alkali derivative compounds are synthesized by structurally modifying the first, third and ninth sites of beta-carboline parent nucleus and importantly introducing amido into the first and third sites; and the obvious anti-tumor activity of the compounds is kept, and the water solubility of the compounds is improved. A method for preparing the compounds is simple and convenient, the yield is high, and the beta-carboline alkali derivative compounds can be used for preparing medicines for treating various tumor diseases.

The invention discloses a compound 1-(4-hydroxy-3-methoxycarbonylphenyl)-beta-carboline-3-formyl-Tyr-Ile-Gly-Ser-Arg, wherein YIGSR is formally short forTyr-Ile-Gly-Ser-Arg. The invention also discloses a preparation method of the compound, a nano-structure of the compound, an anti-tumor effect of the compound, an effect of the compound in inhibiting adhesion, invasion and migration of tumor cells, further discloses antiinflammatory and antithrombotic effects of the compound and expounds an application of the compound in medical science.

The invention discloses a general formula I compound and a general formula II compound having thrombus dissolving activity, a preparation method thereof and an application thereof as thrombus dissolving agent. The invention adopts a rat carotid-jugular vein bypass intubation thrombus model to evaluate the thrombus dissolving activity of the general formula I compound and the general formula II compound respectively. Animal experimental results show that: both the general formula I compound and the general formula II compound have excellent thrombus dissolving activity and can be applied to clinical practice as a thrombus dissolving agent.

Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.

The invention relates to the technical field of medicines and discloses an indoletriazole alkaloid antifungal compound with a novel framework, i.e. fructus evodiae triazole alkali (3-[2-N-methyianiline]-triazolo[4,3-a]-3,4-dihydto-beta-carboline) which is a compound with a brand-new framework. The invention also relates to a preparation method and application of the indoletriazole alkaloid antifungal in the field of medicines. Particularly, the compound has strong antifungal activity, and compared with the antifungal medicaments clinically applied at present, the compound has the advantages of high efficiency, low toxicity, broad antifungal spectrum, and the like, opens a new approach for deeply researching and developing new antifungal medicaments and can be used for preparing new antifungal medicaments.

The invention belongs in the field of organic chemistry and relates to a new shortened Pictet-Spengler type reaction for preparing isomerically pure beta-carboline compounds useful for the synthesis of tadalafil.

The invention relates to beta-carboline derivatives, and a preparation method and the application thereof. More particularly, the invention relates to compounds in formula (I), wherein AA, n, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are defined by the specification. The invention also relates to the preparation method of the compounds shown in the formula (I), a pharmaceutical composition containing the compounds shown in the formula (I), and the application of the compounds to the preparation of antineoplastic drugs. The compounds have special inhibitory activity for the cell proliferationof four cancer cells including K562, HT-29, HL60 and A549.

The invention discloses RGD tetrapeptide modified beta-carboline acyl-tryptophan and discloses a preparation method, a nanostructure, an effect of resisting tumor cell adhesion, an effect of resisting tumor cell invasion, an effect of resisting tumor cell migration, an anti-rumor effect and an effect of inhibiting tumor transfer to lung. The invention discloses application thereof in medicine. The formula is as shown in the specification.

The invention discloses a beta-carboline alkaloid and application thereof to preparing antimalarial medicaments. The structure of the beta-carboline alkaloid is as shown in a formula (I) described in the specification. The beta-carboline alkaloid disclosed by the invention or pharmaceutical salt thereof plays a killing role on plasmodia, can be used for preparing the antimalarial medicaments and treating plasmodium infectious diseases and provides more drug choices for treating malaria. R is expressed in the formula (I), wherein R1=OMe, OH or H.

The invention discloses heterocyclic carboxylic acid-modified thymopentins. The heterocyclic carboxylic acid-modified thymopentins have a general formula I. In the general formula I, RCO represents 1,2,3,4-tetrahydro-beta-carboline-3-formyl, beta-carboline-3-formyl, 1,2,3,4-tetrahydroisoquinol-3-formyl, isoquinol-3-formyl, 1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-formyl, 1-methyl-beta-carboline-3-formyl or 4,5,6,7-tetrahydro-3H-imidazo[4,5-C]pyridyl-6-formyl. The invention also discloses a preparation method of the heterocyclic carboxylic acid-modified thymopentins, and in-vitro tumor cell proliferation-resistant activity of the heterocyclic carboxylic acid-modified thymopentins. The invention further discloses heterocyclic carboxylic acid-modified thymopentin activity of inhibiting weight gain of a tumor in a S180 tumor-loading mice, and use of the heterocyclic carboxylic acid-modified thymopentins in preparation of anti-tumor drugs. The general formula I is RCO-Arg-Lys-Asp-Val-Tyr.

The invention discloses 1-(4-isopropyl propyl)-beta-carboline-3-formyl-Trp-Trp-Trp-Lys-Glu structured as follows, a preparation method therefor, a nanostructure thereof, antitumor action thereof, action thereof in resisting adhesion and invasion and migration of tumor cells, and illustrates application thereof in medical science. The formula is shown in the description.

The invention discloses 13 types of beta-carboline-3-formyl- Orn(ClCH2NH)-AA-NHCH2C6H5 in a following formula (in the formula, AA is selected from L-Arg, L-Asn, L-Asp, L-Glu, L-Gly, L-Ile, L-Leu, L-Met, L-Phe, L-Pro, L-Thr, L-Trp, and L-Val residues), also discloses the preparation methods thereof, discloses the inhibition effect for tumor cells growth, and discloses an application of the substrates as the antitumor drugs.

The invention provides beta-carboline modified by KE as well as preparation, nanostructure, activity and application of the same. The invention discloses 1-(4-hydroxy-3-methoxycarbonyl phenyl)-[beta]-carboline-3-formyl-Lys-Glu having a following structure shown in the description, wherein the standard abbreviation of Lys-Glu is KE, and discloses a preparation method thereof, a nanostructure thereof, an anti-tumor effect thereof, and effects on resisting tumour cells adhering to invade and migrating thereof. Further, the invention discloses anti-inflammatory effect of the same, and explains the application in medical science.

The invention discloses a 3-position diamine connected beta-carboline alkali compound, and a preparation method, a medicinal composition and a use thereof. The above di-beta-carboline alkali compound and its medicinal salt are represented by general formula I, and the preparation method of the di-beta-carboline alkali compound comprises the following steps: carrying out a condensation reaction on two molecules of beta-carboline-3-formaldehyde and one molecule of diamine NH2(CH2)nNH2, and hydrogenating. The invention also discloses the medicinal composition, and an application of the di-beta-carboline alkali compound in the preparation of antitumor medicines. The medicinal composition comprises an effective amount of the di-beta-carboline alkali compound represented by the formula I and a pharmacodynamically acceptable carrier. The antitumor medicines are used for treating melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermal cancer, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer and colon cancer.

The invention discloses a green synthetic method of a beta-carboline compound. The green synthetic method of the beta-carboline compound is technically characterized by comprising the following steps: carrying out Pictet-Spengler reaction on L-tryptophan to prepare tetrahydro-beta-carboline-3-carboxylic acid; and decarboxylating and oxidizing the tetrahydro-beta-carboline-3-carboxylic acid under the effect of an oxidizing decarboxylating agent hydrogen peroxide to prepare the beta-carboline compound. The invention discloses specific synthetic steps and main reaction equations in the preparation process. The method disclosed by the invention has the advantages of simple preparation and safety and environmental-friendliness, and the yield of the beta-carboline compound is high, so that the demand on green chemistry is satisfied.

The invention discloses a copper chloride complex using 1-(2-pyridine)-9-hexyl-beta-carboline as a ligand and a synthesis method and application thereof. A structural formula of the complex is shown as the following formula (I). The synthesis method comprises the steps that the compound shown as a following formula (II) and copper chloride are taken and dissolved in a polar solvent to perform complexing reaction, wherein the polar solvent is selected from one or more of methyl alcohol and ethyl alcohol and one or more of water, acetone, chloroform, dichloromethane and N,N-dimethylformamide. The complex shows the stronger antitumor activity than the ligand and cis-platinum, has a good potential medicinal value and is hopeful for preparation of various antitumor drugs. The structures shown by the formulas (I) and (II) are shown in the description.

The invention relates to the analytical chemistry field, particularly to a method for detecting picrasma quassioides alkali content in picrasma quassioides. The method comprises the following steps: preparing 1-carbomethoxy-Beta-carboline, nigakinone, and metiiylnigakinone standard solutions and drawing a standard curve; drying and smashing picrasma quassioides, and extracting to obtain a solution to be detected; detecting, wherein the detection chromatographic condition is that a C18 chromatographic column is adopted, the column temperature is 20-40 DEG C, the detection wave length is 205-280 nm, acetonitrile is taken as an A phase of a mobile phase while acid water is taken as a B phase of the mobile phase, the flow velocity is 1 mL / minute, and the elution procedures are performed in the way that the volume percent of acetonitrile is changed from 5% to 45% during the period from 0 minutes to 35 minutes, from 45% to 80 % during the period from 35 minutes to 40 minutes, from 80% to 90% during the period from 40 minutes to 50 minutes, and from 90% to 95% during the period from 50 minutes to 60 minutes; computing the content of three kinds of picrasma quassioides alkali as per the standard curve, wherein acids in acid water are phosphoric acid, formic acid or acetic acid, and the volume fraction of acid in acid water is 0.1-1%. The method can be used for the ration of three kinds of picrasma quassioides alkali at one time.

The invention relates to carboxylic acid derivatization beta-carboline and a preparation method of the carboxylic acid derivatization beta-carboline. The method comprises the steps that organic solvent is added into the mixture of 6-methyl-beta carbazoline, metal-salt catalyst and initiator, oxygen is introduced, and after stirring reaction is conducted, the reaction is terminated; filtering is conducted, and solid crude products are collected; further purification of the crude products is conducted through recrystallization and silica gel column chromatography to obtain products. According tothe method, reaction conditions are mild, the application range of substrates is wide, and a large number of beta-carboline derivatives with diversified structures can be obtained.

The invention 1-(4-hydroxyl-methoxycarbonyl phenyl)-beta-carboline-3-formyl-Leu-Pro-Asn-Ile-Ser-Lys-Pro structured as follows, wherein standard abbreviation Leu-Pro-Asn-Ile-Ser-Lys-Pro is LPNISKP. The invention discloses a preparation method therefor, a nanostructure thereof, antitumor action thereof, action thereof in resisting adhesion, invasion and migration of tumor cells and further discloses anti-inflammatory action thereof, and illustrates application thereof in medical science. The formula is shown in t he description.

The invention relates to a beta-carboline compound and a synthetic method and application thereof, and belongs to the technical field of medicine. The structure of the compound is shown as the formula I (the formula I is shown in the specification). After an initial test, it is indicated that the in-vitro anti-renal-fibrosis activity of the compound is remarkable, the treatment effect on renal interstitial fibrosis caused by obstruction of the left ureter of a Balb / c mouse is good, the good potential medical value is achieved, and the beta-carboline compound and the synthetic method and application thereof can be used for preparing various kinds of anti-renal-fibrosis and anti-chronic-kidney-disease medicine.