长春花生物碱类衍生物及靶向前药研究进展

摘要]长春花生物碱作为一类抗有丝分裂药物，能够抑制微管聚合并诱导聚合的微管蛋白解聚。目前主要从两方面对长春碱类药物进行结构修饰：一是依据长春花生物碱类药物的构效关系，对其活性中心进行修饰，合成一系列长春碱类衍生物，以期寻找到具有更高药理活性、更低毒性和更广抗肿瘤谱的长春花生物碱类药物；二是在保证药理活性的前提下，在一些非活性位点引入靶向基团(特异性寡肽、单克隆抗体及叶酸等)，合成一系列长春花生物碱类衍生物靶向前药，以期降低长春碱类药物的毒副作用，提高其治疗指数。文中综述了长春花生物碱类衍生物和长春花生物碱类药物靶向前药的研究进展。

Progress in research of Vinca alkaloids and its targeting prodrugs

Abstract]As a kind of antimitotic drugs,Vinca alkaloids can inhibit microtubule assembly and induce tubulin self-association into coiled spiral aggregates.Currently,the structural modification of Vinca alkaloids is focused mainly on two aspects.One is modification of the biologically active groups according to the structure-activity relationship (SAR) to search for more active and less toxic new analogues with a broader spectrum of anticancer efficacy.Another is to introduce some targeting groups (such as biologically specific oligopeptide, monoclonal antibody and folic acid) in biologically inactive groups, which do not affect their pharmacological efficacy.This modification will lower the toxic and side effects of Vinca alkaloid-type compounds,and improve their therapeutic index.In this paper,we reviewed the progress in research of Vinca alkaloids and their targeting prodrugs.