147 results about "Chalcone derivative" patented technology

The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor / anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and / or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenyl flavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and / or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.

The invention discloses a quinoid chalcone compound with a methyl group at an A ring, and a preparation method and anti-inflammatory activity thereof. The compound has a structure as shown in a general formula (I) which is described in the specification. The preparation method comprises the following steps: (1) synthesizing 2-hydroxy-4,6-dimethoxyacetophenone; (2) synthesizing 2'-hydroxy-4',6'-dimethoxychalcone derivative; (3) synthesizing 2',4',6'-trihydroxy chalcone derivative; and (4) synthesizing the quinoid chalcone compound with a methyl group at the A ring. The compound is simple to prepare and has obvious anti-inflammatory action.

The invention provides a method for preparing derivatives of cis-oximes and oxime ethers. The method comprises the following steps of: dissolving chalcone, chalcone derivatives and hydroxylamine or alcoxyl amine salt in a solvent, adjusting a pH value of the solution to a proper value, and adding a catalyst to obtain the cis-oxime or oxime ether compounds. The method has the advantages of obtaining the cis products by one-step reaction, along with easy and convenient operation and suitability for mass production. The invention also provides the oximes and oxime ethers prepared by the method, and the oximes and oxime ethers have the characteristics of high yield and high purity.

The invention provides a preparation method of a chalcone derivative, relates to an preparation method of a chalcone, and aims at finding the chalcone derivative with the action of an inducer for inducing the apoptosis of the tumor cells. The preparation method of the chalcone derivative comprises: (1) synthesis of 2,6-dimethoxy quinone; (2) synthesis of 2,6-dimethoxy-p-hydroxybenzene; (3) synthesis of 2-hydroxy-4,6-dimethoxy-5-acetyl acetophenone complex; (4) synthesis of 3,6-dihydroxy-2,4-dimethoxy-acetophenone; (5) synthesis of 2-hydroxy-4,5,6-trimethoxy acetophenone; and (6) synthesis of 2',3-dihydroxy-4,4',5',6'-tetramethoxy chalcone. The preparation method provided by the invention is used for the preparation of 2',3-dihydroxy-4,4',5',6'-tetramethoxy chalcone and the inducer used for inducing the apoptosis of the tumor cells.

The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor / anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

The invention discloses a chalcone derivative with good anti-free radical oxidative damage activity. The structural formula of the chalcone derivative is shown as the following. The preparation method of the chalcone derivative includes: letting syringaldehyde and para-substituted acetophenone react in piperidine and under a high temperature so as to generate corresponding substituted chalcone; reacting purified chalcone with sodium borohydride under a cerous chloride heptahydrate condition to generate a chalcone derivative crude product, and then conducting purification. , Compared with ascorbic acid, the product provided by the invention has low anti-DPPH free radical and anti-ABTS<+> free radical IC50 value, and strong free radical scavenging ability, thus having broad application prospects in preparing drugs for treating neurodegenerative diseases. (formula I).

The invention discloses a compound with an effect of resisting plant viruses, namely a preparation method and biological activity for a chalcone derivative containing quinazoline thioether. The preparation method is used for synthesizing chalcone derivative containing quinazoline thioether by using vairous aromatic aldehydes, p-hydroxy phenyl ethyl ketone, o-aminobenzoic acid, formamide, thionyl chloride, potassium hydroxide and potassium carbonate as raw materials through six steps. The compounds M2, M6, M9 and M22 have relatively high protection, passivation and treatment effect to a tobacco mosaic virus (TMV), and can be used for preparing a novel pesticide for preventing plant virus diseases. According to a formula shown in the description, R is a benzene ring, a substituted aromatic ring and a substituted heterocyclic ring, o-position, m-position and p-position on the aromatic ring comprise one or more of methoxy groups, nitryl, methyl, trifluoromethyl, 2-chlorine-5-nitryl as well as halogen atoms; the halogen atoms can be fluorine, chlorine, bromine and iodine; the heterocyclic ring is a five-member ring, a substituted five-member ring or a six-member ring.

The present invention provides 2-hydroxy-3-amino methylene-4, 6-dibubstituted chalcone derivative with the structural general expression as shown. The preparation process includes the following steps: Lewis acid catalyzed reaction of compound I and anhydrous methy1cyanide inside inert solvent to obtain intermediate trihydroxy acetophenone amide hydrochloride; further acid hydrolysis to obtain compound II; selective etherification with alkylation reagent under alkaline cddn to obtain compound III; condensation with aromatic aldehyde under alkaline condition to obtain compound IV; and reaction with secondary amine in the presence of acid and formaldehyde to produce destination compound V. The present invention provides completely new structure compounds with powerful tumor cell inhibiting effect and IC50 value up to 0.8 micron, and capable of being used in preparing antitumor medicine.

Provided is a drug for preventing or improving hyperuricemia which comprises, as the active ingredients, an organic solvent extract or aqueous organic solvent solution extract of at least one plant material selected from the group consisting of artemisia, Saussurea involucrata, chrysanthemum, guava, cudweed (Gnaphalium affine), blue mallow, oregano, Glechoma hederaceae, mentha, Millettia reticulata and peanut, picnogenol and / or a chalcone derivative or glycoside.

The invention discloses a making method of 2'-hydroxy-3'-alkylamino propyl-4', 6'-disubstituted chalcone derivant, which comprises the following steps: adopting 2'-hydroxy chalcone as leading material; proceeding allyl etherifying reaction on the mother core of 2'-hydroxy chalcone; proceeding Claisen rearrangement; epoxidising; additioning; obtaining the product; fitting for industrial manufacturing; improving the receiving rate obviously.

The invention discloses a chalcone derivative containing 1, 1-dichloropropene, a preparation method and application thereof. The derivative has a general formula (I) shown as the specification, wherein R1 is selected from 4-chlorphenyl, 4-fluorophenyl, benzyl, 4-chlorobenzyl and other substituents; R2 is selected from methyl, ethyl, benzyl, 4-chlorobenzyl, ethyl acetate and other substituents. The derivative provided by the invention has the characteristics of simple structure, simple preparation process and low production cost, and has good activity to rice bacterial leaf blight, rice baeterial leaf streak pathogens and caenorhabditis elegans.

The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor / anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

The invention relates to 4,2',4'-triethoxy-5' substituted chalcone derivatives, a preparation method and application of the derivatives to an antitumor medicines. Two compounds refer to 4,2',4'-triethoxy-5' (p-methoxyphenyl) chalcone and 4,2',4'-triethoxy-5' (p-fluorophenyl) chalcone. Two 4,2',4'-triethoxy-5' substituted chalcone derivatives are synthesized for the first time, and the in-vitro tumor cell inhibiting activities of the derivatives are tested. As indicated by results, the derivatives have high inhibiting activity to human erythroleukemia cells (K562) and human colon cancer cells (HT-29).

The invention relates to a preparation method of 5,6,7,4'-tetramethoxy flavone of scutellarin and aglucone key intermediate thereof. The 5,6,7,4'-tetramethoxy flavones is prepared by utilizing 2-hydroxyl-4,5,6-trimethoxy hypnone as the raw material and comprising a reaction a step and a reaction b step, wherein in the reaction a, 2-hydroxyl-4,5,6-trimethoxy hypnone and p-methoxybenzaldehyde are condensed to prepare a chalcone derivative; and in the reaction b, the chalcone derivative is processed in a oxidative cyclization mode to prepare the 5,6,7,4'-tetramethoxy flavone. The method has the advantages of simple operation steps and high product yield.

The invention relates to a pyridine chalcone derivative which has aggregation sate fluorescence enhancement and two-photon fluorescence characteristics and is connected with different aromatic rings or aromatic heteroatomic rings by using allyl acyl-2-pyridyl as a matrix. The pyridine chalcone derivative has a chemical structural formula as shown below, wherein R1 is selected from one of triphenylamine bases, 4-N-carbazole phenyl and 3-(N-ethyl) carbazyl; R2 is selected from one of triphenylamine groups and 4-bromo-triphenylamine group or 3,8-(N-ethyl) carbazyl; and R3 is selected from the triphenylamine group. The pyridine chalcone derivative has important application values in the fields of organic light-emitting diodes (DLED), two-photon fluorescence microscopy, optical switches, biological fluorescence sensors and the like.

The present invention provides an MMP-inhibitory composition comprising chalcone or its derivatives. They inhibit the MMPs in collagenase subfamily as well as those in gelatinase subfamily. The MMP inhibitory activity of chalcone derivatives was similar to or greater than that of parent compound, chalcone. Chalcone or its derivatives of the present invention inhibit activity of matrix metalloproteinase, so that it can be applied to treat and prevent diseases related to matrix metalloproteinase.

The invention discloses a 6-cinnamon acyl-2H-benzo [b] [1, 4] oxazine-3 (4H)-ketone derivative and application thereof, wherein a structural general formula of the derivative is shown in Formula (I), and Ar in the formula represents an aryl. Pharmacological experiments show that the compound provided by the invention has an obviously inhibiting effect on the proliferation of lung carcinoma cells A549, and indicate that a chalcone derivative containing benzoxazine ketone disclosed by the invention has development prospects in clinical applications and has important values in the exploitation of anti-tumor drugs.

The present invention provides novel substituted chalcone derivatives which exhibit anti-hyperglycemic and anti-dyslipedemic activity. The invention also provides a method for treating type II diabetes and associated hyperlipidemic conditions in a mammal by administering the compounds of the present invention and compositions containing these derivatives.

The invention discloses a coumarin-containing chalcone derivative, and a preparation method and an application thereof. The general formula of the derivative is represented by formula (1) shown in thedescription; and in the formula (I), R is a phenyl group, a substituted phenyl group, an aromatic heterocyclic group or a substituted aromatic heterocyclic group, wherein the R being the substitutedphenyl group is a phenyl group substituted with a methyl group, one or more methoxy groups, a trifluoromethyl group, a trifluoromethoxy group or one or more halogen atoms; and the R being the substituted aromatic heterocyclic group is a pyridyl group, a thienyl group, a furyl group or a substituted thiazolyl group. The coumarin-containing chalcone derivative has good inhibitory activity against rice bacterial blight and citrus canker, and the preparation method has the advantages of easily available raw materials, proceeding of a reaction at a low temperature, mild reaction conditions, simplicity in post-treatment, and high yield.

The invention belongs to the technical field of medicinal chemistry, and discloses quatemary ammonium chalcone derivatives resistant to drug-resistance bacteria activities, a preparation method and application of the quatemary ammonium chalcone derivatives. A structural formula is as shown in the description. Proved by invitro antibacterial activity experiments and erythrocyte hemolytic experiments, a large part of compounds in the series of the derivatives have great antibacterial effects and selections on staphylococcus aureus and colonic enterococcus faecalis of gram-positive bacteria, escherichia coli and pseudomonas aeruginosa of gram-negative bacteria. The selected part of compounds show great antimicrobial activities on a plurality of 'superbacteria' including methicillin-resistant staphylococcus aureus (MRSA), vancomycin resistant enterococcus (VRE), carbapenem-resistant enterobacteriaceae (CRE) and new delhi metallo (NDM) carrying NDM genes, and especially show excellent activities on the MRSA. Proved by invitro erythrocyte toxicity experiments, the series of compounds are low in erythrocyte toxicity and can be adopted as new anti-microbial drug candidates.

Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and / or disappearance of the cancer, to the benefit of cancer patients.

The invention provides novel diamino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic and bacteriostatic agents.

The invention belongs to the field of pharmaceutical chemistry, and discloses novel chalcone derivatives with drug-resistant bacteria resistance activity and a synthesis method thereof. The two reaction steps are performed to simply and quickly obtain the target products. The structure of the compounds is disclosed in the specification. The in-vitro antimicrobial activity experiment proves that the compounds have favorable antibacterial activity for methicillin-resistant Staphylococcus aureus (MRSA). The compounds are hopeful to be used as a novel candidate drug for resisting Gram-positive bacteria.

The invention provides a synthesis method of a chalcone derivative, which comprises the following steps: adding polyphosphoric acid PPA and a solvent 1, 4-dioxane into a container, sequentially adding98% concentrated sulfuric acid, substituted benzaldehyde and substituted acetophenone, and performing heating at 90 DEG C under nitrogen protection while stirring to react for 2 hours; and after thereaction is finished, performing separating and purifying to obtain the chalcone derivative. The synthesis method provided by the invention is low in catalyst price, mild in reaction condition, simpleand convenient to operate and high in yield, and a new method is provided for synthesis of a chalcone derivative.

The present invention relates to novel boronic chalcone derivatives which are useful as antitumor / anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic chalcone derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.

The invention discloses a synthetic method for a 1,3,5-triarylbenzene compound. The method comprises the following steps: dissolving a chalcone derivative and inorganic alkali in dimethyl sulfoxide, carrying out reaction at 40 to 80 DEG C in the air for 3 to 8 hours, and carrying out separation and purification so as to obtain the 1,3,5-triarylbenzene compound, wherein a molar ratio of the chalcone derivative to the inorganic alkali is 1: 1-6; every mole of the chalcone derivative requires 4 to 8 mL of dimethyl sulfoxide; and the chalcone derivative has a general structural formula described in the specification, wherein Ar1 and Ar2 are aryl groups. The synthetic method for the 1,3,5-triarylbenzene compound provided by the invention has the following advantages of easily-available raw materials, simple operation, mild reaction conditions, no need of any transition metal catalyst, strong reaction specificity, strong applicability to a basic-group-contained substrate, no generation of waste products like halogen or boric acid, and simple, convenient and green after-treatment.