Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 1, Pages 517-521Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm500362j
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Phosphoinositide 3-kinase gamma (PI3K gamma) is an attractive target to potentially treat a range of disease states. Herein, we describe the evolution of a reported phenylthiazole pan-PI3K inhibitor into a family of potent and selective benzothiazole inhibitors. Using X-ray crystallography, we discovered that compound 22 occupies a previously unreported hydrophobic binding cleft adjacent to the ATP binding site of PI3K gamma, and achieves its selectivity by exploiting natural sequence differences among PI3K isoforms in this region.
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