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Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR |
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| Authors: | Keith A. Menear Sylvie Gomez Karine Malagu Christine Bailey Kristel Blackburn Xiao-Ling Cockcroft Sally Ewen Alexandra Fundo Armelle Le Gall Gesine Hermann Luisa Sebastian Mihiro Sunose Thomas Presnot Eleanor Torode Ian Hickson Niall M.B. Martin Graeme C.M. Smith Kurt G. Pike |
| Affiliation: | 1. KuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK;2. AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK |
| Abstract: | A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series based on a tri-substituted triazine scaffold has led to the discovery of potent and selective inhibitors of mTOR. |
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