The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
作者: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
DOI:10.1016/j.bmcl.2009.08.038
日期:2009.10
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. (C) 2009 Elsevier Ltd. All rights reserved.