Author/Authors :
James P. Edwards، نويسنده , , Robert I. Higuchi، نويسنده , , David T. Winn، نويسنده , , Charlotte L. F. Pooley، نويسنده , , Thomas R. Caferro، نويسنده , , Lawrence G. Hamann، نويسنده , , Lin Zhi، نويسنده , , Keith B. Marschke، نويسنده , , Mark E. Goldman، نويسنده , , Todd K. Jones، نويسنده ,
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 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.
