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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists

Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists

William J Zuercher, Richard G Buckholz, Nino Campobasso, Jon L Collins, Cristin M Galardi, Robert T Gampe, Stephen M Hyatt, Susan L Merrihew, John T Moore, Jeffrey A Oplinger, Paul R Reid, Paul K Spearing, etc.

J Med Chem. 2010 Apr 22;53(8):3412-6.

PMID: 20345102

Abstract:

Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased through iterative analogue synthesis. A ligand-bound cocrystal structure was determined which elucidated key interactions for high binding affinity. Further characterization of the tertiary sulfonamide series led to the identification of high affinity LXR antagonists. GSK2033 (17) is the first potent cell-active LXR antagonist described to date. 17 may be a useful chemical probe to explore the cell biology of this orphan nuclear receptor.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1221277902	GSK2033		1221277-90-2	Price

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