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Communication | Special issue | Vol 76, No. 1, 2008, pp.137-142
Published online, 15th February, 2008
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, and Hiroyuki Miyachi*

*Institute of Molecular and Cellular Biosciences, University of Tokyo, Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan

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.