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

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. doi: 10.1016/s0960-894x(98)00107-3.
J P Edwards 1,  S J West,  C L Pooley,  K B Marschke,  L J Farmer,  T K Jones
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
PMID: 9871534 DOI: 10.1016/s0960-894x(98)00107-3
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.

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