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

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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

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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