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

doi:10.3987/COM-07-S(N)7

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 journal › Article › peer-review

22 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 language	English
Pages (from-to)	137-142
Number of pages	6
Journal	Heterocycles
Volume	76
Issue number	1
DOIs	https://doi.org/10.3987/COM-07-S(N)7
Publication status	Published - 2008
Externally published	Yes

ASJC Scopus subject areas

Analytical Chemistry
Pharmacology
Organic Chemistry

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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.",

author = "Atsushi Aoyama and Hiroshi Aoyama and Kosuke Dodo and Makoto Makishima and Yuichi Hashimoto and Hiroyuki Miyachi",

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T2 - Synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs

AU - Aoyama, Atsushi

AU - Aoyama, Hiroshi

AU - Dodo, Kosuke

AU - Makishima, Makoto

AU - Hashimoto, Yuichi

AU - Miyachi, Hiroyuki

PY - 2008

Y1 - 2008

N2 - 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.

AB - 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.

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

Abstract

ASJC Scopus subject areas

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