New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2 (1H)-pyrrolidino [3, 2-g] quinolinone

JP Edwards, SJ West, CLF Pooley, KB Marschke…

Index: Edwards, James P.; West, Sarah J.; Pooley, Charlotte L. F.; Marschke, Keith B.; Farmer, Luc J.; Jones, Todd K. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 7 p. 745 - 750

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Citation Number: 105

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.