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Bioorg Med Chem Lett. 2012 Sep 15;22(18):5966-70. doi: 10.1016/j.bmcl.2012.07.048. Epub 2012 Jul 21.

Discovery and optimization of a series of liver X receptor antagonists.

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Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA.


The present report describes our efforts to convert an existing LXR agonist into an LXR antagonist using a structure-based approach. A series of benzenesulfonamides was synthesized based on structural modification of a known LXR agonist and was determined to be potent dual liver X receptor (LXR α/β) ligands. Herein we report the identification of compound 54 as the first reported LXR antagonist that is suitable for pharmacological in vivo evaluation in rodents.

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