Acryloylamino-salicylanilides as EGFR PTK inhibitors |
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| Authors: | Deng Wei Guo Zongru Guo Yanshen Feng Zhiqiang Jiang Yi Chu Fengming |
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| Institution: | Department of Synthetic Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China. |
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| 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. |
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