LXR antagonists with a 5-substituted phenanthridin-6-one skeleton: Synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs

Atsushi Aoyama, Hiroshi Aoyama, Kosuke Dodo, Makoto Makishima, Yuichi Hashimoto, Hiroyuki Miyachi

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Conformationally restricted heterocyclic analogs of carba-T0901317, a liver X receptor (LXR) antagonist, were prepared via the palladium catalized cyclization reaction as a key step. In vitro transactivation assay revealed that the structural modification altered the nature of the activity from LXR-agonistic to LXR-antagonistic.

Original languageEnglish
Pages (from-to)137-142
Number of pages6
JournalHeterocycles
Volume76
Issue number1
DOIs
Publication statusPublished - Dec 1 2008

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry

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