Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
P Furet, V Guagnano, RA Fairhurst… - Bioorganic & medicinal …, 2013 - Elsevier
P Furet, V Guagnano, RA Fairhurst, P Imbach-Weese, I Bruce, M Knapp, C Fritsch, F Blasco…
Bioorganic & medicinal chemistry letters, 2013•ElsevierPhosphatidylinositol-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.
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.
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.
Elsevier