喹唑啉类表皮生长因子受体酪氨酸激酶抑制剂药物设计策略

Drug design strategy for quinazoline epidermal growth factor receptor tyrosine kinase inhibitors

表皮生长因子的过表达和突变在肿瘤的形成和发展中起着重要作用,通过抑制表皮生长因子受体介导的信号转导,可以实现对肿瘤的治疗。喹唑啉类小分子靶向表皮生长因子受体酪氨酸激酶抑制剂药物是其中较为活跃的一个研究领域,已有多种药物上市。喹唑啉类衍生物具有较多的结构修饰位点,具有较强的市场开发潜力。对当前喹唑啉类表皮生长因子受体酪氨酸激酶抑制剂药物的发展历程、代表性药物的合成方法、药物构效关系进行了综述,并依据构效关系对喹唑啉类药物的研究前景进行了预测。

Overexpression and mutation of epidermal growth factor play an important role in the formation and development of tumors.Treatment of tumors can be achieved by inhibiting epidermal growth factor receptor-mediated signal transduction.Quinazoline small molecule targeting epidermal growth factor receptor tyrosine kinase inhibitor drugs are one of the more active research fields,and many drugs have been marketed.Quinazoline derivatives have many structural modification sites and have strong market development potential.The development history of quinazoline epidermal growth factor receptor tyrosine kinase inhibitors,the synthesis methods of representative drugs,and the structure-activity relationship of drugs were reviewed,and the research prospect of quinazoline drugs was predicted based on the structure-activity relationship.