多功能铂(Ⅳ)类抗肿瘤药物研究进展

Research Progress of Multifunctional Platinum(Ⅳ)Complexes as Antitumor Agents

癌症是导致人类非正常死亡的主要病因,人类对高效抗癌药物的需求依然迫切。铂类药物是临床上使用最广泛的化疗药物之一,但毒副作用强、吸收率低、靶向性差、耐药性严重等缺陷影响了其临床疗效。铂(Ⅳ)作为新型的铂类药物得到了科研工作者的广泛关注,为新型铂类药物的发展开辟了新方向。目前对于铂(Ⅳ)的开发主要集中于对其轴向配体进行功能化修饰,以制备多功能新型铂(Ⅳ)化合物,按功能可以分为脂水分配调谐型、DNA靶向型、线粒体靶向型、酶靶向型、光动力型铂(Ⅳ)类化合物,相关工作众多。基于此,结合本课题组在铂(Ⅳ)方面的工作基础,文章综述了近三年以来小分子铂(Ⅳ)配合物的研究进展,并分析了其未来的发展趋势,为后续新型铂(Ⅳ)类抗肿瘤药物的研发提供了借鉴与思路。

Cancer is one of the main cause of human death.There is an urgent desire for high effective anticancer drugs in clinic.Platinum drugs are one of the most widely used chemotherapeutic drugs in cancer treatment.However,their clinical efficacy is seriously affected by the strong toxic and side effects,low absorption rate,poor targeting and easily acquired drug resistance.Platinum(Ⅳ),as a new type of platinum drugs,has attracted extensive attention in pharmaceutical field,and opened up a new area for the development of new platinum drugs.At present,the development of platinum(Ⅳ)mainly focuses on the functional modification of its axial ligands to prepare multifunctional new platinum(Ⅳ)compounds.Thees complexes can be divided into lipid water partition tuning,DNA targeting,mitochondrial targeting,enzyme targeting and photodynamic platinum(Ⅳ)compounds based on their functions.Herein,combiningwith authors researches and referring to the works from literatures,this review summarizes the research progress of small molecule platinum(Ⅳ)complexes in recent three years,and the future development trend is also analyzed.This review will provide new reference and ideas for the future development of new platinum(Ⅳ)antitumor drugs.