Substituted 1-[benzofuran-2-yl)-phenylmethyl]-imidazoles as potent inhibitors of aromatase in vitro and in female rats in vivo.

Substituted 1-[(benzofuran-2-yl)-phenylmethyl]-imidazoles are a new class of potent aromatase inhibitor with in vitro IC50 values < 10 nM for certain members using human placental enzyme. At a dose of 2 mg/kg in PMSG-stimulated rats, selected compounds effectively reduce the oestradiol levels by 82-98%.