44 results about "Chalcone derivative" patented technology

The invention belongs to the technical field of medicinal chemistry, and particularly discloses a chalcone derivative and a preparation method thereof.The method includes the steps that 2, 4-dihydroxy formaldehyde serves as an initial raw material, isopentenyl is introduced into 2, 4-dihydroxy benzaldehyde through a Friedel-Crafts reaction, then the 2, 4-dihydroxy benzaldehyde and heterocycle substituted formaldehyde are subjected to an aldol condensation reaction, heterocycle is introduced, a chalcone structure is formed, and the chalcone derivative is obtained. The prepared chalcone derivative has a structural formula as shown in a formula I, physicochemical properties of the chalcone derivative are studied, and the chalcone derivatives I-4, I-5, I-7, I-8, I-9, I-10, I-11, I-12 and I-14 all show relatively strong effects of inhibiting proliferation of four tumor cells (PC9, MDA-MB-231, SMMC-7721 and SGC-7901). The chalcone derivative I-4 can effectively inhibit proliferation of human lung cancer PC9 and H1975 cells, shows concentration dependence, shows good in-vivo anti-tumor activity, can induce ferroptosis of the human lung cancer PC9 and H1975 cells, and has a good application prospect of anti-cancer drugs. # imgabs0 #

The invention discloses a chalcone derivative, the structural formula of the chalcone derivative is as shown in a general formula (1), imgabs0 #. The invention also provides a pharmaceutical composition of the chalcone derivative and application of the pharmaceutical composition, and the newly synthesized compounds show good inhibitory activity through a test on MTHFD inhibitory activity. The invention has important significance for treating MTHFD related diseases, especially lung cancer, colorectal cancer, breast cancer and the like.

The invention discloses application of a chalcone derivative in preparation of a medicine for treating neurodegenerative diseases, belongs to the field of medicines, and researches the neuroprotective effect of a compound (2E)-3-(3, 4-dihydroxyphenyl)-1-(4-methoxyphenyl)-2-propylene-1-ketone by utilizing an oxidative stress model of nerve cells. Experimental results show that the compound can effectively inhibit oxidative stress injury of nerve cells, and a new treatment strategy is provided for treating neurodegenerative diseases.

The application discloses a kind of tetraphenyl ethylene-chalcone derivative preparation and its application preparation and its application.The structure is as follows: the method includes: 4-(1,2,2-triphenyl ethenyl) acetophenone, aldehyde derivative, sodium hydroxide (provides alkaline condition, pH=8.3~8.5), is placed in anhydrous ethanol, under the condition that heating temperature is 80 DEG C, reflux reaction 12h, after reaction is ended, the functional organic material is separated and purified.The functional organic material synthesized according to the above method has larger conjugated system, and has significant pressure-induced color change characteristics.The functional organic material disclosed in the application has low preparation cost, simple operation, simple method, and the material shows significant pressure-induced color change characteristics, can be applied to pressure-induced color change, luminescent material, printing and dyeing, color printing and anti-counterfeiting technical field.

The invention relates to the technical field of villiaumite, in particular to high-purity villiaumite and a preparation method and application thereof. The purity of the high-purity villiaumite is not lower than 99.999%, a photoelectric device modification layer prepared by combining the high-purity villiaumite with a chalcone derivative can effectively regulate and control the wettability of a perovskite precursor solution, growth is induced through a template effect, and finally a perovskite thin film with high crystallinity and a flat surface is obtained. The high-purity villiaumite can effectively avoid impurity defects and promote ordered anchoring of organic molecules to form an ordered structure, so that efficient interface passivation and charge transfer are achieved, and the carrier mobility is improved. The composite modification layer formed by the chalcone derivative and the high-purity villiaumite constructs a stable interface, ion migration and decomposition are effectively inhibited, and the service life of the device is remarkably prolonged.

The invention discloses an active oxygen activated lipoic acid modified chalcone derivative as well as a preparation method and application thereof, and relates to a chalcone derivative as well as a preparation method and application thereof. In order to solve the problems that chalcone lacks tumor selectivity, is insufficient in efficacy and has pharmacokinetics and safety through an ROS anticancer mechanism, the invention comprises three routes: route I: Claisen-Schmidt reaction is combined with Steglich esterification reaction; the route II is as follows: a Claisen-Schmidt reaction is combined with acylating chlorination and Schopper-Baumann esterification; and route 3: arsenic reagent catalytic cyclization is combined with Steglich esterification. The synthesized compound can efficiently and selectively induce cancer cells to generate ROS, exerts excellent anti-cancer activity, reduces oxidative damage to normal tissues to the greatest extent, and provides a new strategy for designing anti-cancer drugs targeting ROS. The invention is applied to the field of medicinal chemistry.

The present invention relates to the field of oncology and provides compounds, compositions, uses and methods for treating cancer, particularly stroma-rich tumors, by selectively targeting cancer-associated fibroblasts (CAFs). CAF targeting is one strategy for enhancing the effectiveness of immunotherapy and can improve the patient response rate. Furthermore, this specificity in the target and related pathways reduces damage to normal tissues.

The present invention discloses a chalcone derivative containing a benzoxazole structure, a preparation method thereof, and an application thereof, and belongs to the field of chemical technology. The present invention uses 1-(4-(3-bromopropyloxy)phenyl)-3-(substituted aromatic)-2-propylene-1-one or 1-(4-(4-bromobutyloxy)phenyl)-3-(substituted aromatic)-2-propylene-1-one to undergo an etherification reaction with benzo[d]oxazole-2-thiol to generate a chalcone derivative containing a benzoxazole structure, the structural formula of which is as follows, wherein n is 3 or 4, and R is any one of a phenyl, a substituted phenyl, a thienyl, or a furyl group. Experimental testing has shown that the derivative has good inhibitory activity against plant bacteria such as rice bacterial blight, melon wilt, and potato soft rot, and can be used as a potential agent for inhibiting plant bacteria.

The invention discloses a preparation method and application of an alkoxy substituted chalcone derivative, and belongs to the field of medicines, the alkoxy substituted chalcone derivative refers to a compound (E)-3-(3, 4-dihydroxyphenyl)-1-(2, 5-dimethoxyphenyl) prop-2-ene-1-ketone, and the structural formula is shown in the specification. The preparation method comprises the following steps: adding 3, 5-dimethoxyacetophenone into a reaction container, adding absolute ethyl alcohol for dissolving, adding a 60% sodium hydroxide aqueous solution, stirring at room temperature, adding 3, 4-dihydroxybenzaldehyde, stirring at 70-90 DEG C for reaction, cooling to room temperature after the reaction is finished, acidifying with hydrochloric acid, extracting with ethyl acetate, drying with anhydrous sodium sulfate, and concentrating under reduced pressure to obtain the 3, 5-dimethoxyacetophenone. And purifying through silica gel column chromatography to obtain a product. The invention also provides application of the alkoxy-substituted chalcone derivative in preparation of drugs for inhibiting oxidative stress injury of nerve cells and application of the alkoxy-substituted chalcone derivative in preparation of drugs for treating neurodegenerative diseases. # imgabs0 #

The application belongs to the field of pharmaceutical chemistry, and provides a carboxyl chalcone derivative and a preparation method thereof, a structural general formula of the carboxyl chalcone derivative is shown in formula (I) or formula (II); in formula (I), R1 is methyl, ethyl, n-propyl, ethynyl, methylamino, dimethylamino, methylthio or methylsulfonyl; in formula (II), R2 is 3-thiophene, 2-thiazole, dihydrobenzofuran, benzodioxolane, benzodioxane, indole, dihydroindole, quinoline or naphthalene. The carboxyl chalcone derivative has excellent inhibitory effect on xanthine oxidase, and can be applied to the preparation of drugs with xanthine oxidase as a target. The application provides more candidate compounds for the development of xanthine oxidase inhibitors.

The application belongs to the technical field of pharmaceutical chemistry, and specifically discloses a chalcone derivative and a preparation method thereof. 2,4-dihydroxy formaldehyde is used as an initial raw material, isopentenyl is introduced into 2,4-dihydroxybenzaldehyde through a Friedel-Crafts reaction, and then a heterocycle is introduced through a hydroxy aldehyde condensation reaction of the heterocycle-substituted formaldehyde, so that a chalcone structure is formed. The prepared chalcone derivative has a structural formula as shown in Formula I, and the physicochemical properties thereof are studied. It is proved that the chalcone derivatives I-4, I-5, I-7, I-8, I-9, I-10, I-11, I-12 and I-14 all show a strong inhibitory effect on the proliferation of four tumor cells (PC9, MDA-MB-231, SMMC-7721 and SGC-7901). Among them, the chalcone derivative I-4 can effectively inhibit the proliferation of human lung cancer PC9 and H1975 cells in a concentration-dependent manner, and shows good in-vivo anti-tumor activity and can induce iron death of human lung cancer PC9 and H1975 cells, and has a good application prospect as an anticancer drug.

The present invention provides a method for preparing a sulfonamido chalcone derivative. Under gold catalysis, a p-toluenesulfonyl structure containing a nitrogen element is used to replace the A-ring structure in chalcone. Under mild reaction conditions, a series of chalcone derivatives containing a sulfonyl structure and having the α-position substituted by a benzene ring or other heterocyclic groups are synthesized through a one-step reaction.

The invention discloses a chalcone compound containing a glycine substituent group or a pharmaceutically acceptable salt thereof as well as a preparation method and application of the chalcone compound, and belongs to the technical field of chalcone derivative preparation, the structural general formula of the chalcone compound containing the glycine substituent group is Ar-C (= O)-CH = C (Ar)-NH-CH2-COOH, wherein Ar and Ar are independently selected from benzene rings with 1-3 substituent groups X, and X is selected from hydrogen, halogen, hydroxyl, methoxyl, nitryl, methyl, carboxyl or amino. According to the chalcone compound containing the glycine substituent, oxidative stress, lipid metabolism disorder and an inflammation pathway are synergistically regulated and controlled, the comprehensive protection effect on alcoholic liver diseases is achieved, the curative effect is better than that of existing clinical drugs, and the chalcone compound containing the glycine substituent has good patent medicine prospects.

The present invention relates to diphenyl ether-based chalcone derivatives, their preparation methods and applications, and belongs to the technical field of chalcone derivatives. The diphenyl ether-based chalcone derivatives of the present invention have a structural formula as shown in formula (I): wherein, R is any one of a halogen atom, a C1-C4-alkyl group, a C1-C4-alkoxy group, a C1-C4-haloalkyl group, a C1-C4-haloalkoxy group, and ; R 0 is any one of a halogen atom, a C1-C4-alkyl group, a C1-C4-alkoxy group, a C1-C4-haloalkyl group, and a C1-C4-haloalkoxy group. The diphenyl ether-based chalcone derivatives provided by the present invention are easy to synthesize, have low cost, and have good inhibitory effects on human bacteria. Formula (I).

Estrogen compounds, compositions, and methods are provided. The novel estrogen compounds include novel chalcone derivatives and analogs that have little or no measurable estrogen (estradiol, E2) activity but enhance E2 activity without binding to the estrogen receptor (ER). The novel compositions comprise one or more novel estrogen compounds, and may optionally comprise one or more excipients. The one or more excipients may be pharmaceutically acceptable. The one or more excipients may include at least one compound that is not present in nature with the estrogen compound. Methods comprise administering to a patient in need of treatment with an estrogen compound or pharmaceutical composition a pharmaceutical composition comprising an estrogen compound described herein.

The application provides an application of a sulfamoyl-based chalcone derivative, the compound contains a methylsulfonyl structure and is substituted by a benzene ring or other heterocyclic groups at an alpha position, has higher inhibiting capability on Hela cells than glycyrrhiza chalcone A, is a compound with significant antitumor activity, and provides a research basis for screening of new antitumor drugs.

The invention belongs to the technical field of synthesis of unsaturated amide derivatives. The invention provides a method for synthesizing an alpha, beta-unsaturated amide derivative, which comprises the following steps: adding a chalcone derivative and methylsulfonyl hydroxylamine trifluoromethanesulfonate into a solvent, and reacting to obtain a product. According to the method provided by the invention, the'one-pot efficient construction of alpha, beta-unsaturated amide from ketene 'is completed directly by chalcone and methylsulfonyl hydroxylamine trifluoromethanesulfonate only under the room temperature condition in which tetrahydrofuran participates', the steps are short, the conditions are mild, expensive or high-toxicity metal and high-temperature dependence are not needed, and the method is suitable for industrial production. And meanwhile, the atom economy is better, the process heat release is controllable, and gram-level and even larger-scale amplification is facilitated.

The invention provides a synthesis method of a benzo [a] fluorene compound. According to the method, o-aryl vinyl substituted cinnamyl aldehyde or o-aryl vinyl substituted chalcone derivatives are used as raw materials, protonic acids or lewis acids such as trifluoromethanesulfonic acid and iron trifluoromethanesulfonate are used as catalysts, reaction is performed for 2-12 hours at the temperature of 50-100 DEG C, reaction liquid is separated and purified, and the benzo [a] fluorene compound shown in the formula (I) is obtained. The synthesis method disclosed by the invention has the characteristics of simplicity and convenience in operation, high atom economy, simplicity in substrate preparation, wide application range and the like, and is suitable for actual organic synthesis.

The application discloses a chalcone derivative with a structure shown in formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof and application thereof as an active ingredient in preparation of an NLRP3 inflammasome inhibitor and / or a STATs pathway inhibitor. The compound can selectively inhibit the activation of the NLRP3 inflammasome and can inhibit the STATs pathway, thereby treating or improving diseases related to the NLRP3 inflammasome and / or the STATs pathway, such as acute peritonitis and colitis, and can be used in preparation of a therapeutic drug for diseases related to the NLRP3 inflammasome and / or the STATs pathway.

The present invention is directed towards catalysts comprising metal nanoparticles and a N-heterocyclic carbene comprising palladium or nickel, their use in carbonylative coupling reactions and hydrogenation reactions, and their use in one-pot carbonylative coupling and hydrogenation reaction. A method employing such catalysts to access ynone and chalcone derivatives is also claimed. The catalysts and methods of the present invention improve upon the disadvantages associated with literature reactions.

The invention relates to a chalcone derivative, a preparation method thereof and application of the chalcone derivative in preparation of an anti-angiogenesis medicine. The molecular structure of the chalcone derivative is shown as a formula I. The chalcone derivative disclosed by the invention can obviously inhibit angiogenesis in a vascular endothelial cell HMEC-1 and a zebra fish body at a relatively low concentration, and can be used as a new chemical entity for preparing a novel anti-angiogenesis medicine.

The invention belongs to the technical field of medicine synthesis, and particularly discloses an aminoalkylated paeonol chalcone derivative as well as a preparation method and medical application thereof. The amine alkylation paeonol chalcone derivative is shown as a general formula (I), and is obtained by taking paeonol as a raw material, connecting phenolic hydroxyl groups on the paeonol with organic amine fragments by utilizing different connecting arms, and then carrying out Claisen-Schmidt condensation with various benzaldehydes. In-vitro anti-tumor experiments prove that the derivative has good anti-tumor activity on human colon cancer cells (HCT116), human hepatoma cells (HepG2), human lung cancer cells (A549) and human osteosarcoma cells (U2OS), has obviously better water solubility than paeonol chalcone, is expected to be developed into a medicine for treating various cancers such as colon cancer, osteosarcoma, lung cancer or liver cancer, and has broad application prospects. The clinical application prospect is wide.

The invention relates to the technical field of cooling liquid, and discloses a composition for preparing the cooling liquid, the cooling liquid as well as a preparation method and application of the cooling liquid. 45 to 55 parts by weight of water; 1-2 parts by weight of a low ionization degree organic acid corrosion inhibitor; 0.5 to 1 part by weight of an azole compound; 0.2 to 0.7 part by weight of an ion trapping agent; 0.1 to 0.5 part by weight of an amine pH regulator; 0.3 to 0.8 part by weight of a chalcone derivative; and 0.5 to 1.2 parts by weight of a nonionic azo ligand compound. The cooling liquid has low conductivity and also maintains excellent corrosion inhibition capability.

The present disclosure provides compounds of formula 1 to inhibit or prevent mitochondrial dysfunction by augmenting mitochondrial function. Mitochondrial dysfunction is the hallmark of a wide range of diseases and disorders. Mitochondria are a promising therapeutic target for the detection, prevention and treatment of various human diseases such as cancer, neurodegenerative diseases, ischemia-reperfusion injury, diabetes and obesity.

The invention discloses a pyrazole-containing chalcone derivative as well as a preparation method and application thereof, and belongs to the technical field of pesticide synthesis. A series of pyrazol-containing chalcone derivatives are synthesized by taking chalcone as a leading structure and introducing a pyrazol skeleton with excellent agricultural activity into the structure of chalcone, and plant pathogenic fungus activity inhibition tests are carried out on the synthesized pyrazol-containing chalcone derivatives, so that the activity of the pyrazol-containing chalcone derivatives is shown in the description. The synthesized pyrazole-containing chalcone derivative can effectively inhibit plant pathogenic fungi, and especially has relatively good inhibitory activity on phomopsis, phytophthora capsici and capsicum oxysporum.

The application provides a fluorescent probe for detecting amyloid oligomers and preparation and application thereof, and belongs to the technical field of A beta imaging agents, wherein the fluorescent probe is a chalcone derivative, and is specifically a chalcone skeleton-based molecular twist limited charge transfer and excited state proton transfer process optimization and development, which can be used as a specific fluorescent chemical probe for detecting and imaging A beta aggregates, and can dynamically monitor A beta aggregates in an in-vitro fiber formation process, and has important significance for A beta related pathological detection and research.

This invention belongs to the field of pharmaceutical synthesis technology, specifically disclosing an aminoalkylated paeonol chalcone derivative, its preparation method, and its pharmaceutical uses. The aminoalkylated paeonol chalcone derivative of this invention is shown in general formula (I). It is obtained by using paeonol as a raw material, linking the phenolic hydroxyl groups on paeonol to organic amine fragments using different linking arms, and then performing Claisen-Schmidt condensation with various benzaldehydes. In vitro antitumor experiments have demonstrated that the derivative of this invention exhibits good antitumor activity against human colon cancer cells (HCT116), human liver cancer cells (HepG2), human lung cancer cells (A549), and human osteosarcoma cells (U2OS), and has significantly better water solubility than paeonol chalcone. It holds promise for development as a therapeutic drug for various cancers such as colon cancer, osteosarcoma, lung cancer, and liver cancer, with broad clinical application prospects.

The present invention relates to: an organic semiconductor compound having a chalcone derivative structure; an organic semiconductor layer comprising same; and an optoelectronic synaptic device capable of discriminating the three primary colors and comprising same. The organic semiconductor compound according to the present invention has large differences in wavelength-specific absorbance in the visible spectrum and exhibits a high dipole moment upon light absorption. Therefore, the conductance induced in a switching medium according to the intensity of applied light can be modulated, and thus an optoelectronic synaptic device capable of discriminating various colors can be achieved by outputting different output signals for red light (R), green light (G), and blue light (B) input signals. In addition, the organic semiconductor compound can exhibit optical synaptic properties regardless of the type of switching medium of a resistive memory device, and the optoelectronic synaptic device using same is a two-terminal memristor-type device and highly integrated.

The invention discloses an application of chalcone derivative psoralen B in preparation of a GPR84 receptor antagonist and a medicine for treating GPR84 receptor related diseases. Cell experiments show that the compound is an antagonist of GPR84 and has concentration dependence; animal experiments show that the compound has a remarkable drug effect on a Crohn disease colitis model induced by 2, 4, 6-trinitrobenzenesulfonic acid (TNBS), and can relieve colon shortening caused by the TNBS and improve the weight loss degree. The compound can be used for preparing a GPR84 antagonist and preventing and treating GPR84 related diseases such as Crohn's disease, non-alcoholic fatty liver disease, reflux esophagitis and the like.

The application discloses a 3'-geranyl-4,2',4',6'-tetrahydroxy dihydrochalcone against gram-positive bacteria, and a chemical structural formula of the dihydrochalcone is shown as formula (I). The application further provides a preparation method and application of the dihydrochalcone derivative. The 3'-geranyl-4,2',4',6'-tetrahydroxy dihydrochalcone has significant antibacterial activity against gram-positive bacteria, MRSA retention bacteria activity, and can significantly inhibit the formation of gram-positive bacterial biofilm.