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
  • 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.