Discovery and Synthesis of a Novel Series of Liver X Receptor Antagonists

Siyun Nian; Xia Gan; Xiangduan Tan; Zhenpeng Yu; Panfeng Wang; Xing Chen; Guoping Wang

doi:10.1248/cpb.c15-00261

Notes

Discovery and Synthesis of a Novel Series of Liver X Receptor Antagonists

Siyun Nian, Xia Gan, Xiangduan Tan, Zhenpeng Yu, Panfeng Wang, Xing Chen, Guoping Wang

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Keywords: liver X receptor α, liver X receptor β, antagonistic activity

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2015 Volume 63 Issue 8 Pages 628-635

DOI https://doi.org/10.1248/cpb.c15-00261

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Abstract

Fourteen novel compounds were prepared and their antagonistic activities against liver X receptors (LXR) α/β were tested in vitro. Compound 26 had an IC₅₀ value of 6.4 µM against LXRα and an IC₅₀ value of 5.6 µM against LXRβ. Docking studies and the results of structure–activity relationships support the further development of this chemical series as LXRα/β antagonists.

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