Nonsteroidal Androgen Receptor Agonists Based on 4-(Trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
2010
Abstract A series of 2 H -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)-2 H -pyrano[3,2- g ]quinolin-2-one displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as mesaured 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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