Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase …

Y Mao, W Zhu, X Kong, Z Wang, H Xie, J Ding…

Index: Mao, Yongjun; Zhu, Wenxiu; Kong, Xiaoguang; Wang, Zhen; Xie, Hua; Ding, Jian; Terrett, Nicholas Kenneth; Shen, Jingkang Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 3090 - 3104

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Citation Number: 13

Abstract

36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino- 3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure– activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an ...

~62%

~89%

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase ...

[Petrov, Kimberly G.; Zhang, Yue-Mei; Carter, Malcolm; Cockerill, G. Stuart; Dickerson, Scott; Gauthier, Cassandra A.; Guo, Yu; Mook Jr., Robert A.; Rusnak, David W.; Walker, Ann L.; Wood, Edgar R.; Lackey, Karen E. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 17 p. 4686 - 4691]

Synthesis and SAR of potent EGFR/erbB2 dual inhibitors

[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]