Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives

…, HJ Brodie, W Garrett, CH Tsai-Morris…

Index: Marsh, David A.; Brodie, Harry J.; Garrett, Wesley; Tsai-Morris, Chon-Hwa; Brodie, Angela M. H. Journal of Medicinal Chemistry, 1985 , vol. 28, # 6 p. 788 - 795

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Citation Number: 118

Abstract

The synthesis and biological evaluation of androstenedione derivatives as inhibitors of estrogen biosynthesis are described. The results show that 4-hydroxy analogues are among the most potent in vitro inhibitors of the series. Esterification of the 4-hydroxy steroids generally reduced activity. Further conjugation of the 3-keto 4-ene system to give 4-hydroxy- 4, 6-androstadiene-3, 17-dione caused more rapid inactivation of aromatase in rat ovarian ...

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