Details

Autor(en) / Beteiligte

• EDWARDS, J. P
• HIGUCHI, R. I
• WINN, D. T
• POOLEY, C. L. F
• CAFERRO, T. R
• HAMANN, L. G
• LIN ZHI
• MARSCHKE, K. B
• GOLDMAN, M. E
• JONES, T. K

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 1999-04, Vol.9 (7), p.1003-1008

Ort / Verlag

Oxford: Elsevier

Erscheinungsjahr

1999

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• 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.