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Bioorg Med Chem Lett. 2012 Jul 15;22(14):4613-8. doi: 10.1016/j.bmcl.2012.05.090. Epub 2012 Jun 5.

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Author information

1
Cellzome Ltd, Chesterford Research Park, Little Chesterford CB10 1XL, UK. sunosem@hotmail.co.jp

Abstract

Herein, we disclose the discovery of a series of 7-substituted triazolopyridines which culminated in the identification of 14 (CZC24758), a potent, orally bioavailable small-molecule inhibitor of PI3Kγ, an attractive drug target for inflammatory and autoimmune disorders. Compound 14 has excellent selectivity across the kinome, demonstrates good potency in cell based assays and furthermore exhibits in vivo efficacy in a collagen induced arthritis model in mouse after oral dosing.

PMID:
22726925
DOI:
10.1016/j.bmcl.2012.05.090
[Indexed for MEDLINE]

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