Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369606 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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.
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Related Topics
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Organic Chemistry
Authors
Mihiro Sunose, Kathryn Bell, Katie Ellard, Giovanna Bergamini, Gitte Neubauer, Thilo Werner, Nigel Ramsden,