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ID: ALA1130772

Journal: Bioorg Med Chem Lett

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

Authors: Edwards JP, West SJ, Pooley CL, Marschke KB, Farmer LJ, Jones TK.

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.

CiteXplore: 9871534

DOI: 10.1016/s0960-894x(98)00107-3