Synthesis and SAR of potent EGFR/erbB2 dual inhibitors

…, SB Guntrip, D Rusnak, K Smith, D Vanderwall…

文献索引：Zhang, Yue-Mei; Cockerill, Stuart; Guntrip, Stephen B.; Rusnak, David; Smith, Kathryn; Vanderwall, Dana; Wood, Edgar; Lackey, Karen Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 1 p. 111 - 114

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被引用次数: 52

摘要

A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC50 values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.