Enhancement of EGFR tyrosine kinase inhibition by C–C multiple bonds-containing anilinoquinazolines

HS Ban, Y Tanaka, W Nabeyama, M Hatori…

文献索引：Ban, Hyun Seung; Tanaka, Yuko; Nabeyama, Wataru; Hatori, Masako; Nakamura, Hiroyuki Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 2 p. 870 - 879

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被引用次数: 24

摘要

A series of 4-anilinoquinazolines with C–C multiple bond substitutions at the 6-position were synthesized and investigated for their potential to inhibit epidermal growth factor receptor (EGFR) tyrosine kinase activity. Among the compounds synthesized, alkyne 6d and allenes 7d and 7f significantly inhibited EGFR tyrosine kinase activity. These compounds inhibited EGF-mediated phosphorylation of EGFR in A431 cells, resulting in cell-cycle arrest and ...