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

  • Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007.
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
  • 1. Novartis Institutes for BioMedical Research, WKL-136.4.12, CH-4002 Basel, Switzerland.
PMID: 23726034 DOI: 10.1016/j.bmcl.2013.05.007
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.