具有抗肿瘤活性的铂类配合物及其作用机制研究进展  

Recent development in platinum complexes with anticancer activities and the underlying mechanisms

作　　者：陈填烽[1] 李林林[1] 禹莲玲[1] 杨芳[1] 郑文杰[1] 

机构地区：[1]暨南大学生命科学技术学院化学系,广东广州510632

出　　处：《暨南大学学报（自然科学与医学版）》2012年第1期94-102,共9页Journal of Jinan University(Natural Science & Medicine Edition)

基　　金：教育部新世纪优秀人才支持计划(NCET10-O119);国家自然科学基金项目(20901030);广东省科技攻关项目(2008A030201020);中央高校基本科研业务费专项资金项目(11610203);华南肿瘤学国家重点实验室开放课题资助

摘　　要：顺铂自二十世纪七十年代起被批准并广泛应用于肿瘤的临床治疗,对多肿瘤疗效显著.但水溶性小、毒副作用大及获得性耐药等缺点极大的限制了铂类配合物的发展与应用.为了获得高效低毒的抗肿瘤药物,科学家们合成了数以千计的铂类配合物,并取得了阶段性进展.本文综述了近五年合成的铂类配合物的结构及其抗肿瘤活性与机制,分成:①具有空间位阻的铂(Ⅱ)配合物;②多核铂(Ⅱ)配合物;③含硫、磷酸(盐)配位原子铂(Ⅱ)配合物;④改变配体或离去基团合成的配合物及⑤铂(IV)配合物等五个类型分别阐述.Cisplatin has been approved and widely used as anticancer drugs in clinical application since 1970s. Although cisplatin exhibited excellent and broad-speetrum antieaneer activities, its low solubility, high toxicity, drug resistanee, and other adverse side effects have limited its clinical applications. To obtain anticaneer complexes 4with high efficacy and low toxicity, scientists have synthesized thousands of platinum complexes and have acquired gradual improvement. This paper reviews the recent developments in platinum were classified as complexes with anticancer activities and the underlying mechanisms. The complexes were classified as ①sterically hindered platinum （Ⅱ） complexes;②multinuclear platinum （Ⅱ） complexes; ③platinum （Ⅱ） complexes with P or S as coordination atom; ④other platinum （Ⅱ） complexes with small ligands; ⑤platinum （Ⅳ） complexes and so on.

关 键 词：抗肿瘤 铂配合物 作用机制 

分 类 号：O614.82[理学—无机化学] R73-36[理学—化学]