Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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Furet, Pascal, Guagnano, Vito, Fairhurst, Robin, Imbach-Weese, Patricia, Bruce, Ian, Knapp, Mark, Fritsch, Christine, Blasco, Francesca, Blanz, Joachim, Aichholz, Reiner, Hamon, Jacques, 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 |