Acryloylamino-salicylanilides as EGFR PTK inhibitors

W Deng, Z Guo, Y Guo, Z Feng, Y Jiang…

Index: Deng, Wei; Guo, Zongru; Guo, Yanshen; Feng, Zhiqiang; Jiang, Yi; Chu, Fengming Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 469 - 472

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Citation Number: 35

Abstract

A series of acryloylamino-salicylanilides were synthesized as inhibitors of EGFR PTK. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bonding in salicylanilides is employed to mimic the planar pyrimidine ring of quinazoline EGFR inhibitors. Acrylamido moiety is incorporated to target the Cys-773 of EGFR specifically. Some of the obtained compounds exhibited good activity as EGFR inhibitors.