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Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14.

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

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1
Novartis Institutes for BioMedical Research, WKL-136.4.12, CH-4002 Basel, Switzerland.

Erratum in

  • Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.

Abstract

Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.

PMID:
23726034
DOI:
10.1016/j.bmcl.2013.05.007
[Indexed for MEDLINE]

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