573982-25-9Relevant articles and documents
Discovery and optimization of a series of liver X receptor antagonists
Jiao, Xianyun,Kopecky, David J.,Fisher, Ben,Piper, Derek E.,Labelle, Marc,McKendry, Sharon,Harrison, Martin,Jones, Stuart,Jaen, Juan,Shiau, Andrew K.,Escaron, Patrick,Danao, Jean,Chai, Anne,Coward, Peter,Kayser, Frank
, p. 5966 - 5970 (2012)
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.