Studies on Aromatase Inhibitors IV. Synthesis and Biological Evaluation of N, N-Disubstituted-5-aminopyrimidine Derivatives.

…, T Yoden, E Kawaminami, Y SHIMADA…

Index: Okada, Minoru; Yoden, Toru; Kawaminami, Eiji; Shimada, Yoshiaki; Kudoh, Masafumi; Isomura, Yasuo Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 8 p. 1293 - 1299

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Citation Number: 11

Abstract

In order to study the potency of the 5-aminopyrimidine skeleton as an aromatase inhibitor, we synthesized various N, N-disubstituted-5-aminopyrimidine derivatives and evaluated their aromatase-inhibitory activity (in vitro) and their inhibitory activity on pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis (in vivo). Compounds with the fluoro-substituted benzyl group showed potent aromatase inhibition. Among them, 5-[(4- ...