A Novel Class of Inhibitors for Human and Rat Steroid 5. ALPHA.-Reductases: Synthesis and Biological Evaluation of Indoline and Aniline Derivatives. III.

S Igarashi, H Inami, H Hara, H Koutoku…

Index: Igarashi; Inami; Hara; Koutoku; Oritani; Mase Chemical and Pharmaceutical Bulletin, 2000 , vol. 48, # 11 p. 1689 - 1697

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Citation Number: 5

Abstract

While searching for novel nonsteroidal inhibitors of human and rat prostatic 5α-reductases, we found a new series of indoline and aniline derivatives that showed potent inhibitory activities for both enzymes. Among them, 3-chloro-4-{1-(4-phenoxybenzyl) indolin-5-yl] oxy} benzoic acid (2e, YM-36117) showed a more portent inhibitory activity for the human enzyme than ONO-3805 with an IC 50 value of 5.3 nM and a reduced rat prostatic ...