2. Academic Validation
  3. Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor alpha antagonists

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

Affiliation

  • 1 Discovery Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan. k2-kikuchi@hhc.eisai.co.jp
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.

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