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Bioorg Med Chem Lett. 1998 Apr 7;8(7):745-50.

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

Author information

1
Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.

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.

PMID:
9871534
[Indexed for MEDLINE]

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