A COMPARISON OF STEROIDAL AND NONSTEROIDAL INHIBITORS OF HUMAN STEROID 5-ALPHA-REDUCTASE - NEW TRICYCLIC ARYL ACID INHIBITORS OF THE TYPE-1ISOZYME

Authors
ABELL AD BRANDT M LEVY MA HOLT DA
Citation
Ad. Abell et al., A COMPARISON OF STEROIDAL AND NONSTEROIDAL INHIBITORS OF HUMAN STEROID 5-ALPHA-REDUCTASE - NEW TRICYCLIC ARYL ACID INHIBITORS OF THE TYPE-1ISOZYME, Bioorganic & medicinal chemistry letters, 6(4), 1996, pp. 481-484
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
4
Year of publication
1996
Pages
481 - 484
Database
ISI
SICI code
0960-894X(1996)6:4<481:ACOSAN>2.0.ZU;2-T
Abstract
A series of 9,10-dihydrophenanthrene-2-carboxylic acids has been prepa red and evaluated in vitro as inhibitors of human recombinant steroid 5 alpha-reductase. 7-Bromo-9,10-dihydrophenanthrene-2-carboxylic acid, 8c, is a potent and selective non-steroidal inhibitor of human type-1 steroid 5 alpha-reductase (K-i,K-app 26 nM). The inhibitory activity relationships of steroidal and non-steroidal inhibitors, with 4-aza, 6 -aza, diene acid, aryl acid and nitro-alkenes functionalities, are con sidered.