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Development of 'DFG-out' inhibitors of gatekeeper mutant kinases |
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| Authors: | Hwan Geun Choi Jianming Zhang Ellen Weisberg James D Griffin Taebo Sim Nathanael S Gray |
| Institution: | Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave, SGM 628, Boston, MA 02115, USA. |
| Abstract: | HG-7-85-01(22) and HG-7-86-01(26) are thiazolo5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I- Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors. |
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