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Bioorg Med Chem Lett. 1999 Apr 5;9(7):1003-8.

Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.

Author information

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

Abstract

A series of 2H-pyrano[3,2-g]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one, displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as measured by an hAR cotransfection assay in CV-1 cells and bound to hAR with high affinity in a whole cell assay. Several analogues were able to activate hAR-mediated gene transcription more potently and efficaciously than dihydrotestosterone.

PMID:
10230628
DOI:
10.1016/s0960-894x(99)00118-3
[Indexed for MEDLINE]

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