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. 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

Pascal Furet  1 , Vito Guagnano, Robin A Fairhurst, Patricia Imbach-Weese, Ian Bruce, Mark Knapp, Christine Fritsch, Francesca Blasco, Joachim Blanz, Reiner Aichholz, Jacques Hamon, Doriano Fabbro, Giorgio Caravatti
Affiliations

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

Pascal Furet et al. Bioorg Med Chem Lett. .

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.

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