Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor alpha antagonists

Bioorg Med Chem Lett. 2001 May 7;11(9):1215-8. doi: 10.1016/s0960-894x(01)00177-9.

Abstract

In the course of studies on novel retinoids, we have designed and synthesized a series of quinoline derivatives. One of them, 4-[5-[8-(1-methylethyl)-4-phenyl-2-quinolinyl]-1H-2-pyrrolyl]benzoic acid (12f) shows potent RARalpha-selective antagonistic activity.

MeSH terms

  • Aldehydes / chemical synthesis
  • Aldehydes / pharmacology
  • Benzoates / chemical synthesis
  • Benzoates / pharmacology
  • Binding, Competitive / drug effects
  • HL-60 Cells
  • Humans
  • Quinolines / chemical synthesis*
  • Quinolines / pharmacology*
  • Receptors, Retinoic Acid / antagonists & inhibitors*
  • Retinoic Acid Receptor alpha
  • Structure-Activity Relationship

Substances

  • Aldehydes
  • Benzoates
  • Quinolines
  • RARA protein, human
  • Receptors, Retinoic Acid
  • Retinoic Acid Receptor alpha