Synthesis and antitumor evaluation of novel 5-substituted-4-hydroxy-8-nitroquinazolines as EGFR signaling-targeted inhibitors

…, HY Li, LP Lin, J Tan, J Ding, X Luo, YQ Long

文献索引：Jin, Yi; Li, Hui-Yuan; Lin, Li-Ping; Tan, Jinzhi; Ding, Jian; Luo, Xiaomin; Long, Ya-Qiu Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 19 p. 5613 - 5622

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被引用次数: 51

摘要

The synthesis and biological activity of a series of novel 5-substituted-4-hydroxy-8- nitroquinazolines that may function as inhibitors of EGFR-and/or ErbB-2-related oncogenic signaling are described. These compounds were prepared by SNAr reaction of 5-chloro-4- hydroxy-8-nitroquinazoline with alkyl or aryl amines, or alkyl alcohol as nucleophiles. Although the enzyme assay showed a weak inhibition effect against both EGFR and ErbB- ...