2. Academic Validation
  3. The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

  • Bioorg Med Chem Lett. 2009 Oct 15;19(20):5950-3. doi: 10.1016/j.bmcl.2009.08.038.
Karine Malagu 1,  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
Affiliations

Affiliation

  • 1 KuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK.
PMID: 19762236 DOI: 10.1016/j.bmcl.2009.08.038
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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