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.
View MoreBrightGene Bio-Medical Technology Co., Ltd.
website:https://en.bright-gene.com/
Contact:+86-512-62551801
Address:Building C25 - C31, No. 218 Xinghu Road, Suzhou Industrial Park, Suzhou, Jiangsu, China.
Chengdu Biopurify Phytochemicals Ltd.
website:http://www.phytopurify.com
Contact:+86-28-82633397
Address:2F,No.11 Building,No.388 Rongtaidadao CNSTP,Wenjiang Zone,Chengdu,Sichuan, China
Xiamen Kaijia Imp & Exp Co., Ltd.
Contact:86-592-5101177
Address:Room406 Luhui Building No. 65 Haitian Road Huli Xiamen,China.
Beijing Harmony Chemical Co., Ltd.
Contact:86-010-84956928
Address:Room 207, Jin feng he B building, No 8 Xin Jie Kou Wai Street, Xi Cheng District, Beijing,PRC. 10008
Sichuan Jisheng BioPharmaceutical Co., Ltd.
website:http://www.jisheng-peptide.com/
Contact:86-833-2598983
Address:No. 3, Jianye Road, High-tech Zone, Leshan City, Sichuan, China
Doi:10.1016/j.tetasy.2004.05.004
(2004)Doi:10.1248/cpb.12.877
(1964)Doi:10.1021/ic00130a026
(1995)Doi:10.1016/0040-4039(95)01162-B
(1995)Doi:10.1039/b817254d
(2009)Doi:10.1021/jo8025274
(2009)