S. Igarashi et al., A novel class of inhibitors for human and rat steroid 5 alpha-reductases: Synthesis and biological evaluation of indoline and aniline derivatives. III, CHEM PHARM, 48(11), 2000, pp. 1689-1697
While searching for novel nonsteroidal inhibitors of human and rat prostati
c 5 alpha -reductases, we found a new series of indoline and aniline deriva
tives that showed potent inhibitory activities for both enzymes. Among them
, 3-chloro-4-{[1-(4-phenosybenzyl)indolin-5-yl]oxy}benzoic acid (2e, YM-361
17) showed a more potent inhibitory activity for the human enzyme than ONO-
3805 with an IC50 value of 5.3 nM and a reduced rat prostatic dihydrotestos
terone (DHT) concentration by oral administration. The synthesis and the st
ructure-activity relationships of these indoline and aniline derivatives ar
e presented.