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化学进展 2012, Vol. Issue (9): 1707-1719 前一篇   后一篇

• 综述与评论 •

抗肿瘤多核铂配合物的研究

徐刚1,2, 姜平元1,2, 苟少华*1,2   

  1. 1. 东南大学化学化工学院 南京 211189;
    2. 江苏省生物药物高技术研究重点实验室 南京 211189
  • 收稿日期:2011-11-01 修回日期:2012-06-01 出版日期:2012-09-24 发布日期:2012-09-27
  • 通讯作者: 苟少华 E-mail:sgou@seu.edu.cn
  • 基金资助:

    国家自然科学基金项目(No. 20971022和No.21271041)资助

Multinuclear Anticancer Platinum Complexes

Xu Gang1,2, Jiang Pingyuan1,2, Gou Shaohua1,2   

  1. 1. School of Chemistry and Chemical Engineering, Nanjing 211189, China;
    2. Jiangsu Province Hi-Tech Key Laboratory for Bio-Medical Research, Nanjing 211189, China
  • Received:2011-11-01 Revised:2012-06-01 Online:2012-09-24 Published:2012-09-27
多核铂配合物作为非经典铂抗肿瘤药物,其抗肿瘤机制与现有铂类抗肿瘤药物不同,因而在克服现有铂类抗肿瘤药物耐药性方面有着巨大的潜力。本文综述了多核铂类抗肿瘤药物的研究进展,以连接铂原子的桥配体结构的不同,可分为六大类:以烷基二胺及其衍生物为桥的多核铂配合物、以含氮杂环为桥的多核铂配合物、以羧酸根为桥的多核铂配合物、以卤素离子为桥的多核铂配合物、以含硫配体为桥的多核铂配合物及以其他配体为桥的多核铂配合物。本文还介绍了这几类多核铂配合物的抗肿瘤机理及在克服顺铂耐药性机理方面的研究进展。
Multinuclear platinum anticancer complexes have been investigated intensively due to their novel structures and promising anticancer activities. Moreover, they are able to overcome cisplatin resistance because of their abilities to form different adducts with DNA compared with those formed by cisplatin. The research status of dinuclear and multinuclear anticancer platinum complexes is reviewed. Based on the different linking ligands, dinuclear and multinuclear are divided to six types, namely, alkyl diamines and their derivatives, heterocyclic compounds containing nitrogen atom(s), carboxylates, haloid anions, ligands containing sulfur atom(s) and other ligands. The possible anticancer mechanism and structure-activity relationship of these multinuclear platinum complexes are also discussed in this paper. Contents 1 Introduction
2 Diamines and their derivatives as linking ligands
2.1 Flexible diamines
2.2 Polyamines
2.3 Semi-rigid diamines and polyamines
3 Heterocycles containing nitrogen atom(s) as linking ligands
3.1 Pyrazole and its derivatives
3.2 Pyrazine and its derivatives
3.3 Bipyridine and its derivatives
3.4 Pyrimidine and its derivatives
3.5 Macrocyclic polyamines
4 Haloid anions as linking ligands
5 Carboxylates as linking ligands
6 Linking ligands containing sulfur atom(s)
7 Other linking ligands
8 Conclusions and outlook

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抗肿瘤多核铂配合物的研究