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Abstract
A series of 4-aryl substituted 7-hydroxy-flavones were prepared using the three-step Baker-Venka-taraman synthesis in good overall yields. The flavones were all evaluated in vitro for inhibitory activity against aromatase (P450AROM/ CYP19), using human placental microsomes, and for inhibitory activity against 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD-1) using human placental cytosol. The phenyl, 4-fluoro-phenyl and 4-bromo-phenyl derivatives displayed moderate inhibitory activity against P450AROM (IC50 17.2, 13.5 and 10.1 μM, respectively), none of the flavones, including the standard genistein, displayed any inhibitory activity against 17β-HSD type 1 at 100 μM concentration.