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.
K Kikuchi  1 ,  K Tagami ,  S Hibi ,  H Yoshimura ,  N Tokuhara ,  K Tai ,  T Hida ,  T Yamauchi ,  M Nagai
Affiliations
PMID: 11354380 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.