Chemical and Pharmaceutical Bulletin p. 382 - 388 (2000)
Update date:2022-08-04
Topics:
Igarashi, Susumu
Inami, Hiroshi
Hara, Hiromu
Fujii, Masahiro
Koutoku, Hiroshi
Oritani, Hiroyuki
Mase, Toshiyasu
In a search for novel nonsteroidal inhibitors of human prostatic 5α- reductase, we found a new series of indole derivatives that showed potent inhibitory activities for the human enzyme. Among them, 4-[(1-benzyl-1- Hindol-5-yl)oxy]-3-chlorobenzoic acid (2d, YM-32906) showed more potent inhibitory activity than finasteride with an IC50 value of 0.44 nM. 3- Chloro-4-{[1-(4-phenoxybenzyl)-1H-indol-5-yl]oxy}benzoic acid (2m) showed inhibitory activities for both human and rat prostatic 5α-reductase with IC50 values of 2.1 and 73 nM, respectively. The synthesis and structure- activity relationships of these indole derivatives are presented.
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