A Novel Class of Inhibitors for Human Steroid 5. ALPHA.-Reductase. Phenoxybenzoic Acid Derivatives. I.

…, H HARA, M FUJII, H KOUTOKU, H ORITANI…

Index: Igarashi, Susumu; Kimura, Takenori; Naito, Ryo; Hara, Hiromu; Fujii, Masahiro; Koutoku, Hiroshi; Oritani, Hiroyuki; Mase, Toshiyasu Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 8 p. 1073 - 1080

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Citation Number: 15

Abstract

In a search for novel nonsteroidal inhibitors of human prostatic 5α-reductase, we found a new series of phenoxybenzoic acid derivatives to be potent human prostatic 5α-reductase inhibitors. Among them, 4-(biphenyl-4-yloxy) benzoic acid derivatives (2n, YM-31758), 2o and 2s showed more potent inhibitory activities than finasteride with IC 50 values of 0.87, 0.67 and 0.56 nM, respectively. The optimized structures for the phenoxybenzoic acid ...