Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure

  • Bioorg Med Chem Lett. 2007 Sep 1;17(17):4808-11. doi: 10.1016/j.bmcl.2007.06.079.
Junichi Sakaki  1 ,  Kazuhide Konishi ,  Masashi Kishida ,  Hiroki Gunji ,  Takanori Kanazawa ,  Hidefumi Uchiyama ,  Hiroaki Fukaya ,  Hironobu Mitani ,  Masaaki Kimura
Affiliations
  • 1. Novartis Institute for Biomedical Research, Tsukuba Research Institute, Ohkubo 8, Tsukuba-Shi, Ibaraki, Japan.
PMID: 17651969 DOI: 10.1016/j.bmcl.2007.06.079
Abstract

Synthesis and structure-activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. Of those antagonists, sulfonamide derivatives (6v and 6w) reveal a high antagonistic activity and good pharmacokinetic properties.