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ACS Med Chem Lett. 2012 May 29;3(7):524-9. doi: 10.1021/ml300045b. eCollection 2012 Jul 12.

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

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Cancer Metabolism Chemistry; Cancer Metabolism Biology; Cancer Metabolism DMPK; Platform Technology Sciences-Computational Chemistry; and Platform Technology Sciences-Screening & Compound Profiling; GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426-0989, United States.


A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under anchorage-independent conditions, and it also demonstrated pharmacodynamic effects and efficacy in a PTEN-deficient prostate cancer PC-3 xenograft mouse model.


PI3K-beta inhibitor; PTEN-deficient; homology model; phosphatidylinositol 3-kinase; structure–activity relationship

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