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 - 2008
Externally publishedYes

Fingerprint

Skeleton
Liver
Cyclization
Palladium
Transcriptional Activation
Assays
Liver X Receptors
TO-901317

ASJC Scopus subject areas

  • Analytical Chemistry
  • Organic Chemistry
  • Pharmacology

Cite this

LXR antagonists with a 5-substituted phenanthridin-6-one skeleton : Synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs. / Aoyama, Atsushi; Aoyama, Hiroshi; Dodo, Kosuke; Makishima, Makoto; Hashimoto, Yuichi; Miyachi, Hiroyuki.

In: Heterocycles, Vol. 76, No. 1, 2008, p. 137-142.

Research output: Contribution to journalArticle

Aoyama, Atsushi ; Aoyama, Hiroshi ; Dodo, Kosuke ; Makishima, Makoto ; Hashimoto, Yuichi ; Miyachi, Hiroyuki. / LXR antagonists with a 5-substituted phenanthridin-6-one skeleton : Synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs. In: Heterocycles. 2008 ; Vol. 76, No. 1. pp. 137-142.
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