Potential aromatase inhibitors and antiestrogen agents based on stilbene and stilbazole derivatives

Abstract

Abstract. Widely used forms of endocrine therapy for women with hormone-dependent breast cancer include blocking the biosynthesis of estrogens through using inhibitors of cytochrome P450 19A1 (aromatase). A series of new stilbene and stilbazole based aromatase inhibitors on are prepared. Z-isomers of 4-(2-(pyridin-4-yl)-1-(1H-1,2,4-triazol-1-yl)vinyl) benzonitrile, 4-(2-(pyridin-3-yl)-1-(1H-1,2,4-triazol-1-yl)vinyl)benzonitrile, 4-(2-(4-fluorophenyl)-1-(1H-1,2,4-triazol1-yl)vinyl)benzonitrile, 4-(2-(4-chlorophenyl)-1-(1H-1,2,4-triazol-1-yl)vinyl)benzonitrile, 4-(2-(4-bromophenyl)-1-(1H-1,2,4triazol-1-yl)vinyl)benzonitrile, 4-(2-(3,4-dimethoxyphenyl)-1-(1H-1,2,4-triazol-1-yl)vinyl)benzonitrile were prepared by condensation of 4-((1H-1,2,4-triazol-1-yl)methyl)benzonitrile and corresponding aldehyde in presence of strong base followed by dehydration of obtained alcohols. Isomerization to corresponded E-isomers was carried out in the presence of UV light.