Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors
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- 作者：Aranapakam M. Venkatesan ; Christoph M. Dehnhardt ; Zecheng Chen ; Efren Delos Santos ; Osvaldo Dos Santos ; Matthew Bursavich ; Adam M. Gilbert ; John W. Ellingboe ; Semiramis Ayral-Kaloustian ; Gulnaz Khafiz
- 关键词：3-Kinase
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 January 2010
- 年：2010
- 卷：20
- 期：2
- 页码：653-656
- 全文大小：354 K
文摘
This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3 K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of Akt at T308.