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

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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