NEW NONSTEROIDAL ANDROGEN RECEPTOR MODULATORS BASED ON 4(TRIFLUOROMETHYL)-2 (1H)-PYRROLIDINO[3,2-G] QUINOLINONE

Authors
EDWARDS JP WEST SJ POOLEY CLF MARSCHKE KB FARMER LJ JONES TK
Citation
Jp. Edwards et al., NEW NONSTEROIDAL ANDROGEN RECEPTOR MODULATORS BASED ON 4(TRIFLUOROMETHYL)-2 (1H)-PYRROLIDINO[3,2-G] QUINOLINONE, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 745-750
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
7
Year of publication
1998
Pages
745 - 750
Database
ISI
SICI code
0960-894X(1998)8:7<745:NNARMB>2.0.ZU;2-M
Abstract
A series of 2(1H)-pyrrolidino [3,2-g]quinolinones was prepared and tes ted for the ability to modulate the transcriptional activity of the hu man androgen receptor (hAR). The parent compound, fluoromethyl)-2(1H)- pyrrolidino[3,2-g]quinolinone, displayed moderate interaction with hAR , but more substituted analogues, particularly 6,7-disubstituted compo unds, were potent hAR agonists in vitro. (C) 1998 Elsevier Science Ltd . All rights reserved.