Discovery and optimization of a novel series of liver X receptor-α agonists

L Li, J Liu, L Zhu, S Cutler, H Hasegawa, B Shan…

Index: Li, Leping; Liu, Jiwen; Zhu, Liusheng; Cutler, Serena; Hasegawa, Hirohiko; Shan, Bei; Medina, Julio C. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1638 - 1642

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Citation Number: 48

Abstract

A novel series of hexafluorocarbinols were discovered as potent activators of the liver X receptor-α using a fluorescence polarization assay. Structure–activity relationship study led to the identification of compounds that are more potent agonists than the endogenous ligand, 24 (S), 25-epoxycholesterol, with similar efficacy. Several compounds, including T0901317, were shown to have desirable pharmacokinetic profiles suitable for in vivo ...