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New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases |
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| Authors: | Mastalerz Harold Chang Ming Chen Ping Dextraze Pierre Fink Brian E Gavai Ashvinikumar Goyal Bindu Han Wen-Ching Johnson Walter Langley David Lee Francis Y Marathe Punit Mathur Arvind Oppenheimer Simone Ruediger Edward Tarrant James Tokarski John S Vite Gregory D Vyas Dolatrai M Wong Henry Wong Tai W Zhang Hongjian Zhang Guifen |
| Affiliation: | Department of Oncology Chemistry, 5 Research Parkway, Wallingford, CT 06492-1951, USA. harold.mastalerz@bms.com |
| Abstract: | Novel C-5 substituted pyrrolotriazines were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The lead compound exhibited promising oral efficacy in both EGFR and HER2 driven human tumor xenograft models. It is hypothesized that its C-5 morpholine side chain binds in the ribose phosphate portion of the ATP binding pocket. |
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