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

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

ACS Med Chem Lett

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.

Published: July 2012

AI Article Synopsis

Article Abstract

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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025772PMC
http://dx.doi.org/10.1021/ml300045bDOI Listing

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