Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR

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• 作者：Keith A. Menear ; Sylvie Gomez ; Karine Malagu ; Christine Bailey ; Kristel Blackburn ; Xiao-Ling Cockcroft ; Sally Ewen ; Alex ; ra Fundo ; Armelle Le Gall ; Gesine Hermann ; Luisa Sebastian ; Mihiro Sunose ; Thom
• 关键词：Mammalian target of rapamycin ; mTOR ; Kinase inhibitors ; Phosphatidylinositol 3-kinase ; PI3K
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 October 2009
• 年：2009
• 卷：19
• 期：20
• 页码：5898-5901
• 全文大小：1398 K

文摘

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.