喹啉类蛋白酪氨酸激酶抑制剂的研究进展

Progressed in quinolines as protein tyrosine kinase inhibitors

蛋白酪氨酸激酶的过度表达与多种肿瘤的发生、发展及转移相关,抑制酪氨酸激酶活性可有效抑制肿瘤。目前已有11个小分子蛋白酪氨酸激酶抑制剂作为抗肿瘤药物上市,1个由美国FDA批准接受预登记的药物,超过100个候选药物处于临床试验阶段。其中喹唑啉结构的酪氨酸激酶抑制剂已成为临床上最常见的抗肿瘤化疗药物类别之一。综述了近年来与喹唑啉结构相似的具有喹啉骨架的酪氨酸激酶抑制剂研究进展。

Protein tyrosine kinases （ PTKs） are closely related with tumor progression. Compounds that inhibit the kinase activity of PTKs are potential chemotherapeutics to treat tumors. Eleven small molecular PTKs inhibitors as anticancer drugs have been approved by FDA. One small molecular has been approved to accept the registration of drugs and over 100 drug candidates are on clinical studies. Three 4-anilinoquinazolines are tyrosine kinase inhibitors （ TKIs） used in the treatment of certain types of cancer and the quinazolines have been of value in cancer chemotherapy. The current review article focuses on the progress of small molecular TKIs featuring a quinoline skeleton similar to the structrue of quinazoline.