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New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone
J P Edwards1, S J West, C L Pooley
1Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
A series of 2(1H)-pyrrolidino[3,2-g]quinolinones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g]quinolinone, displayed moderate interaction with hAR, but more substituted analogues, particularly 6,7-disubstituted compounds, were potent hAR agonists in vitro.