The discovery and optimisation of pyrido[2,3-d
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- 作者：Karine Malagu ; Heather Duggan ; Keith Menear ; Marc Hummersone ; Sylvie Gomez ; Christine Bailey ; Peter Edwards ; Jan Drzewiecki ; Fré ; dé ; ric Leroux ; Mar Jimenez Quesada ; Gesine Hermann ; Stephanie M
- 关键词：Antitumour ; mTOR ; Serine/threonine kinase
- 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：5950-5953
- 全文大小：1689 K
文摘
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.