A Novel Class of Inhibitors for Human and Rat Steroid 5[alpha]-Reductases

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) sho...

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Published inChemical & pharmaceutical bulletin Vol. 48; no. 11; p. 1689
Main Authors IGARASHI, Susumu, INAMI, Hiroshi, HARA, Hiromu, KOUTOKU, Hiroshi, ORITANI, Hiroyuki, MASE, Toshiyasu
Format Journal Article
LanguageEnglish
Published Tokyo Japan Science and Technology Agency 01.11.2000
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Summary: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 IC50 value of 5.3 nM and a reduced rat prostatic dihydrotestosterone (DHT) concentration by oral administration. The synthesis and the structure-activity relationships of these indoline and aniline derivatives are presented.
ISSN:0009-2363
1347-5223