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- W2038471645 abstract "Aromatase (CYP19) catalyzes the aromatization reaction of androgen substrates to estrogens, the last and rate-limiting step in estrogen biosynthesis. Inhibition of aromatase is a new and promising approach to treat hormone-dependent breast cancer. We present here the design and development of isoflavanone derivatives as potential aromatase inhibitors. Structural modifications were performed on the A and B rings of isoflavanones via microwave-assisted, gold-catalyzed annulation reactions of hydroxyaldehydes and alkynes. The in vitro aromatase inhibition of these compounds was determined by fluorescence-based assays utilizing recombinant human aromatase (baculovirus/insect cell-expressed). The compounds 3-(4-phenoxyphenyl)chroman-4-one (1h), 6-methoxy-3-phenylchroman-4-one (2a) and 3-(pyridin-3-yl)chroman-4-one (3b) exhibited potent inhibitory effects against aromatase with IC(50) values of 2.4 μM, 0.26 μM and 5.8 μM, respectively. Docking simulations were employed to investigate crucial enzyme/inhibitor interactions such as hydrophobic interactions, hydrogen bonding and heme iron coordination. This report provides useful information on aromatase inhibition and serves as a starting point for the development of new flavonoid aromatase inhibitors." @default.
- W2038471645 created "2016-06-24" @default.
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- W2038471645 date "2012-04-01" @default.
- W2038471645 modified "2023-10-10" @default.
- W2038471645 title "Development of a new class of aromatase inhibitors: Design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives" @default.
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- W2038471645 doi "https://doi.org/10.1016/j.bmc.2012.02.042" @default.
- W2038471645 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3933949" @default.
- W2038471645 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22444875" @default.
- W2038471645 hasPublicationYear "2012" @default.
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