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Broad spectrum alkynyl inhibitors of T315I Bcr-Abl |
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| Authors: | Xianming Deng Sang Min Lim Jianming Zhang Nathanael S Gray |
| Institution: | 1. Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, and Department of Cancer Biology, Dana-Farber Cancer Institute, 250 Longwood Ave, SGM 628, Boston, MA 02115, United States;2. Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, United States |
| Abstract: | A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC50 of less than 1 nM against wild-type Bcr-Abl and an EC50 of 10 nM against T315I mutant but is broadly active against a number of other kinases. |
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