Document Report Card
Basic Information
ID: ALA1132082
Journal: Bioorg Med Chem Lett
Title: Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
Authors: Edwards JP, Higuchi RI, Winn DT, Pooley CL, Caferro TR, Hamann LG, Zhi L, Marschke KB, Goldman ME, Jones TK.
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.
CiteXplore: 10230628