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.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Androgen Antagonists / chemical synthesis
  • Androgen Antagonists / chemistry
  • Androgen Antagonists / pharmacology*
  • Anilides / chemistry
  • Anilides / pharmacology
  • Animals
  • Cell Line
  • Drug Design
  • Flutamide / chemistry
  • Flutamide / pharmacology
  • Gene Expression Regulation / drug effects
  • Humans
  • Molecular Structure
  • Nitriles
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology*
  • Quinolines / chemical synthesis
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Quinolones / chemical synthesis
  • Quinolones / chemistry
  • Quinolones / pharmacology*
  • Receptors, Androgen / genetics*
  • Recombinant Proteins / biosynthesis
  • Structure-Activity Relationship
  • Tosyl Compounds
  • Transcription, Genetic / drug effects*
  • Transfection

Substances

  • Androgen Antagonists
  • Anilides
  • Nitriles
  • Pyrrolidines
  • Quinolines
  • Quinolones
  • Receptors, Androgen
  • Recombinant Proteins
  • Tosyl Compounds
  • Flutamide
  • bicalutamide