铂类抗肿瘤配合物的研究进展  

Advances in Research on Platinum-based Anticancer Complexes

作　　者：朱阳 程珺洁 刘扬中[1] ZHU Yang;CHENG Junjie;LIU Yangzhong(Department of Chemistry,University of Science and Technology of China,Hefei 230026,China)

机构地区：[1]中国科学技术大学化学与材料科学学院,安徽合肥230026

出　　处：《药学进展》2020年第4期243-255,共13页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.21877103)。

摘　　要：铂类药物因抗癌谱广、疗效显著而在临床中被广泛使用。自1978年顺铂应用于临床以来,卡铂、奥沙利铂相继被美国FDA批准,乐铂、奈达铂和依铂分别在中国、日本以及韩国上市。然而,铂类药物的毒副作用和耐药性大大限制了其应用和开发。为提高铂类药物的疗效以及克服其缺陷,大量的新型铂类配合物被设计合成,并在不同阶段开展疗效试验。除与顺铂类似的铂(Ⅱ)配合物之外,近年来作为前药的铂(Ⅳ)配合物也被广泛研究。从铂(Ⅱ)配合物和铂(Ⅳ)配合物2个方面,总结近年来铂类抗肿瘤配合物取得的研究进展,并对配体的选择与配合物设计、作用机制、抗肿瘤效果以及临床应用前景进行概述,以期对今后的新药开发和临床应用有所裨益。Platinum complexes are widely used in clinical practice because of their extensive anticancer activities and remarkable therapeutic effects.Cisplatin was first put into clinical application in 1978,and later carboplatin and oxaliplatin were successively approved by the FDA.Since then,leplatin,nidaplatin and epplatin have been marketed in China,Japan and Korea,respectively.However,the toxic and side effects and drug resistance of platinum drugs have greatly limited their application and further development.In order to improve the therapeutic efficacy of platinum drugs and overcome their defects,a large number of novel platinum complexes have been designed and synthesized,and the efficacy of some platinum complexes has been evaluated at different stages.In addition to the Pt(II)analogues of cisplatin,Pt(IV)complexes have also been extensively investigated as prodrugs in recent years.In this review,the progress of platinum anti-tumor complexes in recent years is summarized from Pt(II)and Pt(IV)complexes.The design of ligands,the mechanisms,the antitumor effects,and clinical prospects are also discussed.It is expected that this work could be useful for the development and clinical application of platinum-based anticancer drugs in the future.

关 键 词：铂类配合物 抗肿瘤 毒副作用 耐药性 药物设计 

分 类 号：O614.82[理学—无机化学] R918[理学—化学]