Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases |
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| Authors: | Fink Brian E Norris Derek Mastalerz Harold Chen Ping Goyal Bindu Zhao Yufen Kim Soong-Hoon Vite Gregory D Lee Francis Y Zhang Hongjian Oppenheimer Simone Tokarski John S Wong Tai W Gavai Ashvinikumar V |
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| Institution: | Department of Oncology Chemistry, Discovery Biology, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, United States Department of Computer Aided Drug Design, Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, United States |
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| Abstract: | A novel series of 5-((4-aminopiperidin-1-yl)methyl)-pyrrolo2,1-f]1,2,4]triazin-4-amines with small aniline substituents at the C4 position were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. Compound 8l exhibited promising oral efficacy in both EGFR and HER2-driven human tumor xenograft models. |
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| Keywords: | EGFR HER2 Kinase inhibitor |
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