Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.
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Zhi L, Tegley CM, Marschke KB, Jones TK
Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.
Bioorg Med Chem Lett. 1999 Apr 5;9(7):1009-12.
- PubMed ID
- 10230629 [ View in PubMed]
- Abstract
New nonsteroidal human androgen receptor (hAR) agonists were developed from an hAR antagonist pharmacophore, 2(1H)-piperidino[3,2-g]quinolinone. (+/-)-trans-7,8-Diethyl-4-trifluoromethyl-2(H)-piperidino-[3,2-g]quinoli none was synthesized and demonstrated potent hAR agonist activity (EC50=3 nM) in the cell-based cotransfection assay and high binding affinity (Ki=16 nM) in the competitive receptor binding assay.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Stanolone Androgen receptor EC 50 (nM) 6 N/A N/A Details Stanolone Androgen receptor Ki (nM) 2 N/A N/A Details Stanolone Androgen receptor IC 50 (nM) >10000 N/A N/A Details