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

Furet, Pascal and Guagnano, Vito and Fairhurst, Robin and Imbach-Weese, Patricia and Bruce, Ian and Knapp, Mark and Fritsch, Christine and Blasco, Francesca and Blanz, Joachim and Aichholz, Reiner and Hamon, Jacques and Fabbro, Doriano and Caravatti, Giorgio (2013) Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorganic and Medicinal Chemistry Letters, 23 (13). pp. 3741-3748. ISSN 0960-894X

Abstract

Phosphatidylinositol-3-kinase alpha (PI3Kalpha) 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 PI3Kalpha, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.

Item Type: Article
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Keywords: PI3Kalpha NVP-BYL719
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Date Deposited: 13 Oct 2015 13:13
Last Modified: 13 Oct 2015 13:13
URI: https://oak.novartis.com/id/eprint/9380

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