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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.

Author information

1
Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA. xjiao@amgen.com

Abstract

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.

PMID:
22901900
DOI:
10.1016/j.bmcl.2012.07.048
[Indexed for MEDLINE]

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