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小分子蛋白酪氨酸激酶抑制剂的合成研究进展
引用本文:赵迎春,张前军,卢永仲,陈海燕.小分子蛋白酪氨酸激酶抑制剂的合成研究进展[J].化学研究,2014(4):428-440.
作者姓名:赵迎春  张前军  卢永仲  陈海燕
作者单位:[1]贵州大学化学与化工学院,贵州贵阳550025 [2]贵州理工学院药学院,贵州贵阳550007
基金项目:贵州省自然科学基金([2011]2067)
摘    要:蛋白酪氨酸激酶在肿瘤的形成和增殖中起着关键作用,以蛋白酪氨酸激酶作为肿瘤治疗靶点的研究受到极大关注.本文作者综述了近十年来不同结构的酪氨酸激酶抑制剂的合成以及抗肿瘤活性的研究进展,以期为酪氨酸激酶抑制剂的研究与开发提供参考.

关 键 词:酪氨酸激酶抑制剂  合成  生物活性  研究进展

Research progress in synthesis of small molecule protein tyrosine kinase inhibitors
ZhAO Yingchun,ZhANG Qianjun,LU Yongzhong,CHEN Haiyan.Research progress in synthesis of small molecule protein tyrosine kinase inhibitors[J].Chemical Research,2014(4):428-440.
Authors:ZhAO Yingchun  ZhANG Qianjun  LU Yongzhong  CHEN Haiyan
Institution:1 .College of Chemistry and Chemical Engineering, Guizhou University, Guiyang 550025, Guizhou, China ; 2. School of Pharmaceutical Engineering, Guizhou Institute of Technology, Guiyang 550007, Guizhou, China)
Abstract:Protein tyrosine kinase as a target for tumor therapy has gained great attention.In particular,it plays a key role in tumor formation and proliferation.This review focuses on the progress in the synthesis and anti-tumor activity evaluation of protein tyrosine kinase inhibitor with different structures since 2003,with the hope to provide reference for the study and development of protein tyrosine kinases inhibitor in future.
Keywords:tyrosine kinase inhibitors  synthesis  bioactivity  research progress
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