Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinolines

Citation
Jw. Kong et al., Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinolines, BIOORG MED, 10(5), 2000, pp. 411-414
Citations number
29
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
5
Year of publication
2000
Pages
411 - 414
Database
ISI
SICI code
0960-894X(20000306)10:5<411:EOIPRI>2.0.ZU;2-J
Abstract
A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoro methylpyrido[3,2-g]quinolines was synthesized. Compounds in this series wer e tested for the ability to bind to hAR and inhibit hAR-dependent transcrip tion in a mammalian cellular background. (C) 2000 Published by Elsevier Sci ence Ltd. All rights reserved.