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

Bioorganic & Medicinal Chemistry Letters · 2013 · Vol. 23(13) · pp. 3741–3748

Pascal Furet(Novartis (Switzerland))Vito Guagnano(Novartis Institutes for BioMedical Research)Robin A. Fairhurst(Novartis Institutes for BioMedical Research)Patricia Imbach‐Weese(Novartis Institutes for BioMedical Research)Ian C. Bruce(Novartis Institutes for BioMedical Research)Mark Knapp(Novartis (Switzerland))Christine Fritsch(Novartis (Switzerland))Francesca Blasco(Novartis Institutes for BioMedical Research)Joachim Blanz(Novartis (Switzerland))Reiner Aichholz(Novartis (Switzerland))Jacques Hamon(Novartis Institutes for BioMedical Research)Doriano Fabbro(Novartis Institutes for BioMedical Research)Giorgio Caravatti✉(Novartis Institutes for BioMedical Research)

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PI3K/AKT/mTOR signaling in cancer Protein Kinase Regulation and GTPase Signaling Biochemical and Molecular ResearchChemistryPhosphatidylinositolKinaseDrug discoveryPharmacologyPotencyPI3K/AKT/mTOR pathwayAlpha (finance)In vitroBiochemistry

MeSH terms

Phosphoinositide-3 Kinase InhibitorsAnimalsBiological AvailabilityCell LineDogsDose-Response Relationship, DrugFemaleHumansModels, MolecularPhosphorylationStructure-Activity RelationshipThiazolesMolecular StructureRats, Sprague-DawleyPhosphatidylinositol 3-Kinases

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463

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12.26

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99%

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