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

Bioorg Med Chem Lett. 1999 Apr 5;9(7):1003-8. doi: 10.1016/s0960-894x(99)00118-3.

J P Edwards ¹, R I Higuchi, D T Winn, C L Pooley, T R Caferro, L G Hamann, L Zhi, K B Marschke, M E Goldman, T K Jones

Affiliations

Affiliation

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

PMID: 10230628 DOI: 10.1016/s0960-894x(99)00118-3

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.

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