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Studies on aromatase inhibitors. III. Synthesis and biological evaluation of [(4-bromobenzyl)(4-cyanophenyl)amino]azoles and their azine analogs.

作者信息

Okada M, Yoden T, Kawaminami E, Shimada Y, Kudoh M, Isomura Y

机构信息

Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1997 Mar;45(3):482-6. doi: 10.1248/cpb.45.482.

DOI:10.1248/cpb.45.482
PMID:9085555
Abstract

A series of [(4-bromobenzyl)(4-cyanophenyl)amino]azoles and their azine analogs, which have the side chain of the selective aromatase inhibitor YM511, were synthesized and evaluated for aromatase-inhibitory activity (in vitro) and for pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis inhibitory activity (in vivo). Among these aza-heterocycles, the pyrimidin-5-yl derivative (6a) was the most potent aromatase inhibitor and its in vitro inhibitory activity was comparable to that of YM511. Compound 6a also showed weak inhibitory activity on aldosterone synthesis. These data indicated that the pyrimidin-5-yl moiety is useful as a new azole fragment in place of the 4H-1,2,4-triazol-4-yl moiety of the aromatase inhibitor YM511.

摘要

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