New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.

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Edwards JP, West SJ, Pooley CL, Marschke KB, Farmer LJ, Jones TK

New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):745-50.

PubMed ID

9871534 [ View in PubMed

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Abstract

A series of 2(1H)-pyrrolidino[3,2-g]quinolinones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g]quinolinone, displayed moderate interaction with hAR, but more substituted analogues, particularly 6,7-disubstituted compounds, were potent hAR agonists in vitro.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bicalutamide	Androgen receptor	IC 50 (nM)	157	N/A	N/A	Details
Bicalutamide	Androgen receptor	Ki (nM)	82	N/A	N/A	Details
Stanolone	Androgen receptor	EC 50 (nM)	6	N/A	N/A	Details
Stanolone	Androgen receptor	Ki (nM)	2	N/A	N/A	Details