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 2007
Externally publishedYes

Fingerprint

Glucosidases
Thalidomide
Liver
Inhibitory Concentration 50
Liver X Receptors
5-chloro-N-2'-n-pentylphenyl-1,3-dithiophthalimide

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

Cite this

Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors. / Noguchi-Yachide, Tomomi; Miyachi, Hiroyuki; Aoyama, Hiroshi; Aoyama, Atsushi; Makishima, Makoto; Hashimoto, Yuichi.

In: Chemical and Pharmaceutical Bulletin, Vol. 55, No. 12, 12.2007, p. 1750-1754.

Research output: Contribution to journalArticle

Noguchi-Yachide, T, Miyachi, H, Aoyama, H, Aoyama, A, Makishima, M & Hashimoto, Y 2007, 'Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors', Chemical and Pharmaceutical Bulletin, vol. 55, no. 12, pp. 1750-1754. https://doi.org/10.1248/cpb.55.1750
Noguchi-Yachide, Tomomi ; Miyachi, Hiroyuki ; Aoyama, Hiroshi ; Aoyama, Atsushi ; Makishima, Makoto ; Hashimoto, Yuichi. / Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors. In: Chemical and Pharmaceutical Bulletin. 2007 ; Vol. 55, No. 12. pp. 1750-1754.
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