Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
Article Details
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Edwards JP, Higuchi RI, Winn DT, Pooley CL, Caferro TR, Hamann LG, Zhi L, Marschke KB, Goldman ME, Jones TK
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.
- PubMed ID
- 10230628 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bicalutamide Androgen receptor EC 50 (nM) 157 N/A N/A Details Bicalutamide Androgen receptor IC 50 (nM) >10 N/A N/A Details Bicalutamide Androgen receptor IC 50 (nM) 117 N/A N/A Details Stanolone Androgen receptor EC 50 (nM) 6 N/A N/A Details Stanolone Androgen receptor IC 50 (nM) >10 N/A N/A Details Stanolone Androgen receptor IC 50 (nM) 4 N/A N/A Details