Steroids

Probing the binding pocket of the active site of aromatase with 2-phenylaliphatic androsta-1, 4-diene-3, 17-dione steroids

M Takahashi, K Yamashita, M Numazawa

Index: Takahashi, Madoka; Yamashita, Kouwa; Numazawa, Mitsuteru Steroids, 2010 , vol. 75, # 4-5 p. 330 - 337

Full Text: HTML

Citation Number: 10

Abstract

A series of 2-phenylaliphatic-substituted androsta-1, 4-diene-3, 17-diones (6) as well as their androstenedione derivatives (5) were synthesized as aromatase inhibitors to gain insights of structure–activity relationships of varying the alkyl moiety (C1 to C4) of the 2- phenylaliphatic substituents as well as introducing a methyl-or trifluoromethyl function to p- position of a phenethyl moiety to the inhibitory activity. The inhibitors examined showed a ...