New dual inhibitors of EGFR and HER2 protein tyrosine kinases |
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| Authors: | Fink Brian E Vite Gregory D Mastalerz Harold Kadow John F Kim Soong-Hoon Leavitt Kenneth J Du Karen Crews Donald Mitt Toomas Wong Tai W Hunt John T Vyas Dolatrai M Tokarski John S |
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| Affiliation: | Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, NJ 08543-4000, USA. brian.fink@bms.com |
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| Abstract: | 
A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities. |
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