Indole derivatives as a new class of steroid 5α-reductase inhibitors

H Takami, H Koshimura, N Kishibayashi…

文献索引：Takami, Hitoshi; Koshimura, Hirokazu; Kishibayashi, Nobuyuki; Ishii, Akio; Nonaka, Hiromi; Aoyama, Shiro; Kase, Hiroshi; Kumazawa, Toshiaki Journal of Medicinal Chemistry, 1996 , vol. 39, # 26 p. 5047 - 5052

全文：HTML全文

被引用次数: 21

摘要

A series of indole derivatives with varied substituents on the α, β-unsaturated double bond were synthesized and evaluated for their ability to inhibit rat prostatic 5α-reductase. Compounds possessing an ethyl substituent at the β-position of the double bond showed potent inhibitory activity. Among them,(Z)-4-{2-[[3-[1-(4, 4'-difluorobenzhydryl) indol-5-yl]-2- pentenoyl] amino] phenoxy} butyric acid (16, KF20405) showed the maximum potency ...