2. Academic Validation
  3. Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure

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

Affiliation

  • 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.

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