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SAR Studies Around a Series of Triazolopyridines as Potent and Selective PI3Kγ Inhibitors

SAR Studies Around a Series of Triazolopyridines as Potent and Selective PI3Kγ Inhibitors

Kathryn Bell, Mihiro Sunose, Katie Ellard, Andrew Cansfield, Jess Taylor, Warren Miller, Nigel Ramsden, Giovanna Bergamini, Gitte Neubauer

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5257-63.

PMID: 22819766

Abstract:

Herein we describe the SAR of a novel series of 6-aryl-2-amino-triazolopyridines as potent and selective PI3Kγ inhibitors. The 6-aryl-triazolopyridine core was identified by chemoproteomic screening of a kinase focused library. Rapid chemical expansion around a bi-functional core identified the key features required for PI3Kγ activity and selectivity. The series was optimized to afford 43 (CZC19945), a potent PI3Kγ inhibitor with high oral bioavailability and selectivity over PI3Kα and PI3Kδ. Modification to the core afforded 53 (CZC24832) which showed increased selectivity over the entire kinome in particular over PI3Kβ.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1159824675	CZC24832		1159824-67-5	Price

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