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The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase |
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| Authors: | Karine Malagu Heather Duggan Keith Menear Marc Hummersone Sylvie Gomez Christine Bailey Peter Edwards Jan Drzewiecki Frédéric Leroux Mar Jimenez Quesada Gesine Hermann Stephanie Maine Carrie-Anne Molyneaux Armelle Le Gall James Pullen Ian Hickson Lisa Smith Sharon Maguire Niall Martin Graeme Smith Martin Pass |
| Institution: | 1. KuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK;2. AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK |
| Abstract: | We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity. |
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