84212-46-4

Upstream product

• 90-24-4 2-hydroxy-4,6-dimethoxyacetophenone 
• 480-66-0 2,4,6-trihydroxyacetophenone 
• 33495-30-6 2-benzoyloxy-4,6-dimethoxyacetophenone 
• 33507-94-7 1-(2-hydroxy-4,6-dimethoxyphenyl)-3-phenylpropane-1,3-dione 
• 480-40-0 5,7-dihydroxy-2-phenyl-chromen-4-one 
• 105-39-5 chloroacetic acid ethyl ester 
• 21392-57-4 Dimethyl-chrysin 
• 617-33-4 ethyl dibromoacetate 
• 105-36-2 ethyl bromoacetate 

Downstream Products

• 920430-49-5 2-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)-N-(pyridin-2-yl)acetamide 

Relevant academic research and scientific papers

Synthesis of Novel Vindoline-Chrysin Hybrids

Vinca alkaloids are well-known microtubule targeting agents, which are used against some types of cancer. Vindoline is one of the monomeric Vinca alkaloids which does not have anti-tumor effect, although its derivatives have serious impact on the field of

Long-chain primary amide white poplar derivative as well as preparation method and application thereof

The invention belongs to the field of medicines, and relates to a long-chain primary amide chrysin derivative and a preparation method and application thereof. The long-chain primary amide white poplar derivative has the structure shown I, and in the form

Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer

Histone deacetylases (HDACs) inhibitors have demonstrated a great clinical achievement in hematological malignancies. However, the efficacy of HDACs inhibitors in treating solid tumors remains limited due to the complicated tumor microenvironment. In this study, we designed and synthesized a class of novel HDACs inhibitors based on the structure of flavones and isoflavones, followed by biological evaluation. To be specific, a lead compound 15a was discovered with strong anti-proliferative effects on a variety of solid tumor cells, especially for breast cancer cells with resistance to SAHA. Studies demonstrated that 15a could significantly inhibit the activity of HDAC 1, 2, 3 (class I) and 6 (class IIB), leading to a dose-dependent accumulation of acetylated histones and α-Tubulin, cell cycle arrest (G1/S phase) and apoptosis in breast cancer cells. Furthermore, the lead compound 15a could also antagonize the activation of STAT3 induced by HDACs inhibition in some breast cancer cells, which further reduced the level of pro-survive proteins in tumor cells and enhanced anti-tumor activity regulated by STAT3 signaling in vivo. Overall, our findings demonstrated that the novel compound 15a might be a HDACs inhibitor candidate, which could be used as promising chemotherapeutic agent for breast cancer.

Chrysin amide derivative as well as preparation method and medical application thereof

The invention relates to the technical field of pharmaceutical chemistry and in particular relates to a chrysin amide derivative as well as a preparation method and medical application of the derivative. A structural formula of the chrysin amide derivativ

Flavonoid compound and application thereof to anti-cancer medicine

The invention provides a flavonoid compound and application thereof to an anti-cancer medicine. The compound is of a structure of formula (I) shown in the specification, wherein m is 1 to 10; R1 and R2 are respectively selected from hydrogen, hydroxyl, and unsubstituted aryl and heteroaryl or aryl and heteroaryl which are substituted by one or more first substituent groups; X is selected from hydrogen, hydroxyl, nitryl, halogen, amino or cyano; R3 is selected from hydrogen, hydroxyl and -O(CH2)nN(R4R5); n is 2 to 10; R4 and R5 are respectively selected from hydrogen, unsubstituted C1-C10 alkylor C1-C10 alkyl which is substituted by one or more second substituent groups, C2-C12 alkenyl, C1-C10 halogenated alkyl, C2-C12 halogenated alkenyl, C2-C14 heteroalkyl, C2-C12 alkeneoxy, C1-C6 alkyneoxy, amino, C1-C10 alkyl amino, C1-C10 amino alkyl, C1-C10 alkyl carbonyl, C1-C10 carbalkoxy, C1-C10 alkyl amino carbonyl, C1-C10 alkyl carbonyl or C5-C12 aryl carbonyl.

C-7 modified flavonoids as novel tyrosyl-tRNA synthetase inhibitors

Twenty C-7 modified flavonoids were designed and synthesized. Biological evaluation in vitro indicated that compounds generated by SYBYL-X with high scores also showed good inhibitory activities against TyrRS. Compounds containing the nargenin core exhibi

A chrysin preparation of amino acid derivatives (by machine translation)

The invention discloses a chrysin amino acid derivative and its preparation method, dialogue chrysin 7 bit synthesizing different series of chrysin derivatives, the specific synthetic route for chrysin first with supplies immunoglobulin molecules thickener of ester reaction, obtained after the hydrolysis of 7 - O - carboxysomes alkylation chrysin derivatives, with different types of amino acid alkyl ester salt reaction, through the amide condensation to obtain chrysin amino acid alkyl esters, then hydrolyze chrysin amino acid derivatives. The invention relates to amino acid with the chrysin molecule, on the one hand improve the solubility of the chrysin, on the one hand and the killing effect of the normal cell; amino acid is the basic unit of a protein, as an important active molecule in the human body, the process involved in various life activities, non-toxic and harmless to the human body; amino acid has good solubility, and tumor cells to amino acid than normal cell high demand. (by machine translation)

Synthesis and anti-inflammatory in vitro, in silico, and in vivo studies of flavone analogues

Chrysin and 7-hydroxy flavone were prepared by Baker-Venkatraman rearrangement followed by esterification at 7th position and replacement of ester with acetamide linking to different heterocyclic moieties synthesized 13a-g and 14a-g series of flavones analogues. These were screened against COX-2 and COX-1 enzymes for inhibition by in vitro assay and COX-2 for in silico docking studies. The compound 14a was found to be most active with IC50 of 3.11 μM concentration, with highest binding energy of -12.4 kcal/mole and 77.2 and 80.5 % inhibition at 3 and 5 h post-carrageenan induced in paw oedema.

Synthesis, biological evaluation of chrysin derivatives as potential immunosuppressive agents

A series of novel chrysin derivatives was firstly synthesized and evaluated on their immunosuppressive activity in the search for potential immunosuppressive agents. Among them, compounds 5c displayed the most potent immunosuppressive inhibitory activity with IC50 of 0.78 μM, which was comparable to that of cyclosporin A (IC50 = 0.06 μM). The preliminary mechanism of compound 5c inhibition effects was also detected by flow cytometry (FCM), and the compound exerted immunosuppressive activity via inducing the apoptosis of activated lymph node cells in a dose dependent manner. Furthermore, the estimated LD50 (in mg/kg) in vivo of compound 5c is 738.2, which indicated that compound 5c was low toxic.

Furoxan nitric oxide donor coupled chrysin derivatives: Synthesis and vasculoprotection

A series of furoxan-based nitric oxide-releasing chrysin derivatives were synthesized. Pharmacological assays indicated that all chrysin derivatives exhibited in vitro inhibitory activities against aldose reductase and advanced glycation end-product formation. Some chrysin derivatives were also found to increase the glucose consumption of HepG2 cells. Furthermore, the compounds released a low amount of NO in the presence of l-cysteine (range from 0.20% to 1.89%). These hybrid furoxan-based NO donor chrysin derivatives offer a mutual prodrug design concept for the development of therapeutic or preventive agents for vascular complications due to diabetes.