42220-80-4

Upstream product

• 118-93-4 o-hydroxyacetophenone 
• 86-51-1 2,3-dimethyoxybenzaldehyde 

Downstream Products

• 1030592-46-1 2-(2,3-dimethoxyphenyl)-4-(2-hydroxyphenyl)-2,3-dihydro-1H-1,5-benzodiazepine 
• 97207-23-3 2,3-dihydro-2-(2,3-dimethoxyphenyl)chromen-4-one 
• 111017-66-4 (Z)-2(2,3-dimethoxybenzylidene)benzofuran-3(2H)-one 

Relevant academic research and scientific papers

Chalcone compound with anti-tumor activity and preparation method and application thereof

The invention discloses a chalcone compound with anti-tumor activity and a preparation method and application thereof, and belongs to the technical field of medicine synthesis and application. The preparation method comprises the following steps of synthe

Potentiation of Δf508- and G551D-CFTR-mediated Cl- current by novel hydroxypyrazolines

The most common mutation of CFTR, affecting approximately 90% of CF patients, is a deletion of phenylalanine at position 508 (F508del, ΔF508). Misfolding of ΔF508-CFTR impairs both its trafficking to the plasma membrane and its chloride channel activity. To identify small molecules that can restore channel activity of ΔF508-CFTR, we synthesized and evaluated eighteen novel hydroxypyrazoline analogues as CFTR potentiators. To elucidate potentiation activities of hydroxypyrazolines for ΔF508-CFTR, CFTR activity was measured using a halide-sensitive YFP assay, Ussing chamber assay and patch-clamp technique. Compounds 7p, 7q and 7r exhibited excellent potentiation with EC50 value 50 values of 0.88 ± 0.11 and 4.45 ± 0.31 μM for wild-type and ΔF508-CFTR, respectively. In addition, CP7q significantly potentiated chloride conductance of G551DCFTR, a CFTR gating mutant; its maximal potentiation activity was 1.9 fold higher than the well-known CFTR potentiator genistein. Combination treatment with CP7q and VX-809, a corrector of ΔF508-CFTR, significantly enhanced functional rescue of ΔF508-CFTR compared with VX-809 alone. CP7q did not alter the cytosolic cAMP level and showed no cytotoxicity at the concentration showing maximum efficacy. The hydroxypyrazolines may be potential development candidates for drug therapy of cystic fibrosis.

Correlating experimental electrochemistry and theoretical calculations in 2′-hydroxy chalcones: The role of the intramolecular hydrogen bond

In this work we present a study on the molecular structure and electrochemical behavior of a series of methoxylated 2′-hydroxychalcones, whose antitumor activity has been previously described. Cyclic voltammetry was used to quantitatively characterize the

A novel chalcone derivative and composition for anticancer comprising the same

The present invention relates to a novel chalcone derivative and an anticancer composition including the chalcone derivative. In the present invention, provided are an anticancer drug for treating ovarian cancer cells and another anticancer drug for treating ovarian cancer cells having resistance to cisplatin. For this, in the present invention, provided is a compound denoted by chemical formula 1 in which R^1 is H or OCH_3, R^2 is OCH_3 or H, R^3 is OCH_3, R^4 is H, R^5 is OCH_3, R^6 is H and R^7 is OCH_3.

Aurones as histone deacetylase inhibitors: Identification of key features

In this study, a total of 22 flavonoids were tested for their HDAC inhibitory activity using fluorimetric and BRET-based assays. Four aurones were found to be active in both assays and showed IC50 values below 20 μM in the enzymatic assay. Molecular modelling revealed that the presence of hydroxyl groups was responsible for good compound orientation within the isoenzyme catalytic site and zinc chelation.

Aspergillus niger catalyzes the synthesis of flavonoids from chalcones

Flavonoids, which have many biological activities and have been widely used in nature, can be artificially synthesized. However, regioselective cyclization of chalcones is difficult by chemical methods. In this study, we demonstrated that Aspergillus nige

Synthesis of chiral flavanones from tricarbonyl (η6- Arylbenzaldehyde)chromium(0)

A synthesis of chiral flavanones via the condensation of tricarbonyl(η6-arylbenzaldehyde)chromium(0) and o-hydroxyacetophenone in a shorter time at room temperature have been developed. The tricarbonylchromium(0) group was removed by virtue of light and the enantioenriched flavanones was formed with highly enantioselectivity (> 95 % ee).

1H and 13C NMR spectral assignments of 2′-hydroxychalcones

Chalcones are of interest to medicinal chemists because their structures can be easily modified with various functional groups. The syntheses and biological activities of chalcones from natural sources are well known. In this study, 24 2′-hydroxychalcones bearing methoxy substituents were synthesized, among which five are new. The NMR data for all synthesized chalcones are described for the first time. The complete assignments of the 1H and 13C NMR data can be used for the identification of newly discovered and widely isolated, synthesized chalcones. Copyright

Synthesis of 1,5-benzodiazepines with unusual substitution pattern from chalcones under solvent-free microwave irradiation conditions

1,5-Benzodiazepines have been synthesized from the corresponding 2'-hydroxychalcones [1-(2-hydroxyphenyl)-3-aryl-2-propen-1-ones] and o-phenylenediamine, both in methanol, under reflux and under solvent-free microwave irradiation conditions on alumina. Th

Inhibitory activity of prostaglandin E2 production by the synthetic 2′-hydroxychalcone analogues: Synthesis and SAR study

A series of 2′-hydroxychalcones has been synthesized and screened for their in vitro inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells. Structure-activity relationship study suggested that inhibitory activity against prostaglandin E2 production was governed to a greater extent by the substituent on B ring of the chalcone, and most of the active compounds have at least two methoxy or benzyloxy groups on B ring. The relationship between chalcone structures and their PGE2 inhibitory activities was also interpreted by docking study on cyclooxygenase-2.