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

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

Affiliation

  • 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.

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