35794-88-8

Upstream product

• 457930-31-3 4-Methoxy-benzoic acid 2-(4-methoxy-phenyl)-4-oxo-4H-chromen-6-yl ester 
• 76323-08-5 1-acetyl-1,3-bis(benzoyloxy)benzene 
• 100-07-2 4-methoxy-benzoyl chloride 
• 490-78-8 2,5-Dihydroxyacetophenone 
• 794-94-5 p-Methoxybenzoic anhydride 
• 121-98-2 methyl 4-methoxybenzoate 
• 131341-58-7 2,5'-dihydroxy acetophenone 
• 1431642-63-5 1-(2,5-dihydroxyphenyl)-3-(4-methoxyphenyl)propane-1,3-dione 
• 64-19-7 acetic acid 
• 1311272-33-9 2'-hydroxy-5'-(methoxymethoxy)-4-methoxychalcone 
• 107139-52-6 [2-(2,5-Bis-benzoyloxy-phenyl)-2-oxo-ethyl]-triphenyl-phosphonium; bromide 
• 686311-93-3 C₂₄H₂₀O₇ 
• 123-11-5 4-methoxy-benzaldehyde 
• 107127-93-5 1-(2,5-Dihydroxy-phenyl)-2-(triphenyl-λ⁵-phosphanylidene)-ethanone 

Downstream Products

• 139652-32-7 6-[6-(4-hydroxypiperidinyl)hexoxy]-(4-methoxyphenyl)-4H-1-benzopyran-4-one 
• 139652-15-6 6-[5-(4-hydroxypiperidinyl)pentoxy]-2-(4-methoxyphenyl)-4H-1-benzopyran-4-one 

Relevant academic research and scientific papers

Chromanone compound as well as preparation method and application thereof

The invention discloses a chromanone compound, a preparation method of the chromanone compound and application of the chromanone compound to preparation of medicines for treating or preventing infectious diseases caused by mycobacterium tuberculosis. Specifically, the present invention relates to a compound represented by formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound of the present invention, where X, Y, R1, R2, R3 and R4 are as described in the specification. The purpose of the present invention is to prepare a novel compound having anti-mycobacterium tuberculosis activity, which can be used as a potential novel drug for overcoming the problems associated with mycobacterium tuberculosis drug resistance.

Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis

A series of 4H-chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluation showed that compound 8d displayed favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability. An in vivo study indicated that compound 8d exhibited modest efficacy in an acute mouse model of TB after 3 weeks of treatment. Thus, 8d is a promising antituberculosis lead compound.

An Efficient One-Pot Synthesis and Anticancer Activity of 4'-Substituted Flavonoids

A number of 4'-substituted (R = H, Me, Cl, F) flavone derivatives is synthesized from 2-hydroxyacetophenones using the modified Baker–Venkataraman reaction. Compound [3-(4-fluorobenzoyl)-5- hydroxy-4'-fluoroflavone] was synthesized for the first time with the yield of 12%. Antiproliferative assays indicate that the synthesized flavones with F substituent at the 4' position demonstrate higher activity than the other flavone derivatives, particularly against HeLa and MCF-7 with the IC50 9.5 and 2.7 μM, respectively.

Biological activity evaluation and molecular docking study of chromone derivatives as cyclooxygenase-2 inhibitors

A series of chromone derivatives have been evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. The four most potent compounds, 48, 41, 39, and 35 displayed IC50 values of 3.30, 6.86, 7.36 and 7.46 μM, respectively. Compounds 35 and 38 showed higher selectivity for COX-2 (selectivity index, SI = 7.48 and 5.46, respectively) than celecoxib (SI = 4.17 in the same test) whereas compound 39 showed comparable selectivity (SI = 4.19) to celecoxib. The molecular volumes of compounds 35 (312.84 ?3) and 38 (314.18 ?3) were similar to celecoxib (299.28 ?3) but larger than ibuprofen (211.83 ?3). Docking results were in good agreement with the experimental biological data in terms of evaluation of binding energy and binding mode. Compounds 35, 38, and 39 had higher binding affinity against COX-2 (binding energy between ?9.77 and ?11.42 kcal/mole) than COX-1 (binding energy between ?6.28 and ?7.88 kcal/mole). These three chromone compounds also displayed active conformation in the same orientation as that of celecoxib. Thus, compounds in this series has the potential to be a new class of selective COX-2 inhibitor.

Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists

Farnesoid X receptor (FXR), a nuclear receptor mainly distributed in liver and intestine, has been regarded as a potential target for the treatment of various metabolic diseases, cancer and infectious diseases related to liver. Starting from two previously identified chalcone-based FXR antagonists, we tried to increase the activity through the design and synthesis of a library containing chalcones, flavones and chromenes, based on substitution manipulation and conformation (ring closure) restriction strategy. Many chalcones and four chromenes were identified as microM potent FXR antagonists, among which chromene 11c significantly decreased the plasma and hepatic triglyceride level in KKay mice.

Process for the preparation of flavone derivatives

The invention relates to a process for the preparation of flavone derivatives in which a 2-hydroxyacetophenone compound is metallated using a lithium compound at low temperatures and subsequently reacted with a keto compound, and where the ratio of the mo

(Aminoalkoxy)chromones. Selective ? Receptor Ligands

A series of (aminoalkoxy)chromones has been prepared, members of which bind potently (16-100 nM) at the ? binding site and bind weakly (>1000 nm) at the dopamine D2 receptor and 33 other receptors, second messenger systems, and ion channels.At

SYNTHESE DE DIHYDROXY PHENACYLIDENE TRIPHENYLPHOSPHORANES NOUVEAUX PRECURSEURS DE COMPOSES FLAVONOIDES : SYNTHESE D'HYDROXY-6 ET HYDROXY-7 CHROMONES.

The synthesis of two new dihydroxy phenacylidene triphenylphosphoranes from 2,4-dibenzoyloxy and 2,5-dibenzoyloxy acetophenones is described.By acylation of the hydroxyl groups of these ylides, intramolecular olefination of the ester carbonyl group and hydrolysis of the second ester group, some 6-hydroxy and 7-hydroxy chromones are prepared with good yields.

Phytochemical Investigation of Cassia spectablis Seeds Isolation and Structural Studies of Two New Flavone Glycosides

From the seeds of Cassia spectablis 6-hydroxy-4'-methoxy flavone-6-O-arabinopyranoside and 3,5-dihydroxy-7,3',4'-trimethoxy flavone-3-O-arabinopyranoside have been isolated and their structure elucidated. - Key words: Cassia Spectablis, Leguminosae, Flavo