Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors

Tomomi Noguchi-Yachide, Hiroyuki Miyachi, Hiroshi Aoyama, Atsushi Aoyama, Makoto Makishima, Yuichi Hashimoto

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 μM for LXRα and LXR β, respectively.

Original languageEnglish
Pages (from-to)1750-1754
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Volume55
Issue number12
DOIs
Publication statusPublished - Dec 1 2007

Keywords

  • Antagonist
  • Glucosidase inhibitor
  • Liver X receptor
  • Phthalimide skeleton
  • Thalidomide

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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