Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone

Authors
Zhi, L Tegley, CM Marschke, KB Jones, TK
Citation
L. Zhi et al., Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone, BIOORG MED, 9(7), 1999, pp. 1009-1012
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
7
Year of publication
1999
Pages
1009 - 1012
Database
ISI
SICI code
0960-894X(19990405)9:7<1009:SARATA>2.0.ZU;2-W
Abstract
New nonsteroidal human androgen receptor (hAR) agonists were developed from an hAR antagonist pharmacophore, 2(1H)-piperidino[3,2-g]quinolinone. (+/-) -trans-7,8-Diethyl-4-trifluoromethyl-2(1H)-piperidino[3,2-g]quinolinone was synthesized and demonstrated potent hAR agonist activity (EC50 = 3 nM) in the cell-based cotransfection assay and high binding affinity (K-i = 16 nM) in the competitive receptor binding assay. (C) 1999 Elsevier Science Ltd. All rights reserved.