35244-11-2Relevant articles and documents
Preference for O-demethylation reactions in the oxidation of 2′-, 3′-, and 4′-methoxyflavones by human cytochrome P450 enzymes
Nagayoshi, Haruna,Murayama, Norie,Tsujino, Masaki,Takenaka, Shigeo,Katahira, Jun,Kim, Vitchan,Kim, Donghak,Komori, Masayuki,Yamazaki, Hiroshi,Guengerich, F. Peter,Shimada, Tsutomu
, p. 1158 - 1169 (2020)
2′-, 3′-, and 4′-Methoxyflavones (MeFs) were incubated with nine forms of recombinant human cytochrome P450 (P450 or CYP) enzymes in the presence of an NADPH-generating system and the products formed were analyzed with LC-MS/MS methods. CYP1B1.1 and 1B1.3
Synthesis and antiviral activity of 2-aryl-4H-chromen-4-one derivatives against Chikungunya virus
Badavath, Vishnu N.,Jadav, Surender S.,Pastorino, Boris,De Lamballerie, Xavier,Sinha, Barij N.,Jayaprakash, Venkatesan
, p. 1019 - 1024 (2016/11/25)
A series of nineteen 2-aryl-4H-chromen-4-one derivatives 2a-2s were synthesized and evaluated for their antiviral activity against Chikungunya virus (LR2006-OPY1) in Vero cell culture by CPE reduction assay. Three compounds 2a, 2b and 2g, were found to be active at concentration of (IC50) 0.44 μM, 0.45 μM and 2.02 μM, respectively. Compounds having heterocyclic ring 2a and 2b at the 2nd position of the chromenone were found to be potent inhibitor of ChikV. Cytotoxicity studies were performed using Vero cell culture, compounds 2a and 2b exhibited SI of ≥100. Molecular docking simulation has been carried out to understand the possible mechanism of action.
Monoamine oxidase inhibitory activity of 2-aryl-4H-chromen-4-ones
Nayak, Badavath Vishnu,Ciftci-Yabanoglu,Bhakat, Soumendranath,Timiri, Ajay Kumar,Sinha, Barij N.,Ucar,Soliman, Mahmoud E. S.,Jayaprakash, Venkatesan
, p. 72 - 80 (2015/02/19)
A series of twenty 2-aryl-4H-chromen-4-one (flavones) derivatives (3a-3s) were synthesized and tested for hMAO inhibitory activity. Fifteen compounds (3a, 3c, 3e-3h, 3j-3p, 3r, 3s) were found to be selective towards MAO-B, while 3d was selective towards MAO-A, and 3b, 3i and 3q were non-selective. Experimental Selectivity Index for MAO-B ranges from 2.0 (3g, 3p) to 30.0 (3j). Compound 3j, which is carrying 3,4-di-OMeC6H3 groups at R position on the molecule, was found to be potent MAO-B inhibitor amongst the fifteen with Ki value for MAO-B of 0.16 ± 0.01 lM comparable to that of standard drug, Selegiline (Ki for MAO-B is 0.16 ± 0.01 μM). Compound 3j also appeared as the most selective MAO-B inhibitor according to its best selectivity index (30.0), which is comparable to that of Selegiline (SIMAO-B = 35.0). Molecular docking and molecular dynamics simulation studies were carried out using Autodock-4.0 and Amber12 to understand the molecular level interaction and energy relation of MAO isoforms with selective inhibitors (3d and 3j). Simulation results are in good agreement with the experimental results. Leads identified may further be explored to develop potent isoform specific inhibitors of MAO.
