Thirteen 3-phenylchroman-4-ones (isoflavanones) with various substituents at the C6 position or with fluorine modification were synthesized utilizing the gold catalyzed annulation reaction. These compounds were characterized by 1H NMR, 13C NMR and HRMS. The purity of each compound was established by HPLC analysis. The inhibitory potencies against aromatase by these isoflavanones were tested using a fluorescence assay. Docking poses of active isoflavanone inhibitors were predicted by computer modeling.

New selective nonsteroidal aromatase inhibitors: Synthesis and inhibitory activity of 3-phenylchroman-4-ones

243rd National Meeting (2012)

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