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Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors |
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| Authors: | 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 Khafizova Natasja Brooijmans Robert Mallon Irwin Hollander Larry Feldberg Judy Lucas Ker Yu Jay Gibbons Robert Abraham Tarek S Mansour |
| Institution: | 1. Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States;2. Oncology, Wyeth Research, Pearl River, NY 10965, United States |
| Abstract: | 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. |
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