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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

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.