Potential aromatase inhibitors and antiestrogen agents based on stilbene and stilbazole derivatives
https://doi.org/10.29235/1561-8331-2020-56-1-81-87
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.
About the Authors
S. V. Adamchyk
Institute of Bioorganic Chemistry of the National Academy of Sciences of Belarus
Belarus
Belarus
Siarhei V. Adamchyk – Researcher
5/2, Cuprevich Str., 220141, Minsk
A. L. Michal’chuk
Institute of Bioorganic Chemistry of the National Academy of Sciences of Belarus
Belarus
Belarus
Alexander L. Michal’chuk – Ph. D. (Chemistry), Leading Researcher
5/2, Cuprevich Str., 220141, Minsk
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