期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 2, 页码 781-785出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.100
关键词
EGFR; HER2; Kinase inhibitor
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 81 exhibited promising oral efficacy in both EGFR and HER2-driven human tumor xenograft models. (C) 2010 Elsevier Ltd. All rights reserved.
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