Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371087 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A novel series of 5-((4-aminopiperidin-1-yl)methyl)-pyrrolo[2,1-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.
Graphical abstractA novel series of 5-((4-aminopiperidin-1-yl)methyl)-pyrrolo[2,1-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.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Brian E. Fink, Derek Norris, Harold Mastalerz, Ping Chen, Bindu Goyal, Yufen Zhao, Soong-Hoon Kim, Gregory D. Vite, Francis Y. Lee, Hongjian Zhang, Simone Oppenheimer, John S. Tokarski, Tai W. Wong, Ashvinikumar V. Gavai,