A NONSTEROIDAL DIENE ACID INHIBITOR OF HUMAN TYPE-2 STEROID 5-ALPHA-REDUCTASE

Authors
ABELL AD BRANDT M LEVY MA HOLT DA
Citation
Ad. Abell et al., A NONSTEROIDAL DIENE ACID INHIBITOR OF HUMAN TYPE-2 STEROID 5-ALPHA-REDUCTASE, Bioorganic & medicinal chemistry letters, 4(19), 1994, pp. 2327-2330
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
19
Year of publication
1994
Pages
2327 - 2330
Database
ISI
SICI code
0960-894X(1994)4:19<2327:ANDAIO>2.0.ZU;2-Z
Abstract
A series of 4a-methyl-3,4,4a,9-tetrahydrophenanthrene-2- carboxylic ac ids and 2-phosphinic acids has been prepared and evaluated in vitro as inhibitors of human recombinant steroid 5 alpha-reductase. hloro-4a-m ethyl-3,4,4a,9-tetrahydrophenanthrene-2- acid, 5, is a marginally sele ctive inhibitor of human type 2 steroid Sa-reductase (K-i,K-app = 260 nM). The phosphinic acid compounds, 8 and 9, are weak inhibitors of ty pes 1 and 2 steroid 5 alpha-reductase.