金属抗癌药物设计的新策略和新趋势  

New Strategies and Trends for the Design of Metal-Based Anticancer Drugs

作　　者：王晓勇[1] 郭子建[2] 

机构地区：[1]医药生物技术国家重点实验室南京大学生命科学学院,南京210093 [2]配位化学国家重点实验室南京大学化学化工学院,南京210093

出　　处：《化学进展》2009年第5期845-855,共11页Progress in Chemistry

基　　金：国家自然科学基金项目(No.30870554)资助

摘　　要：金属药物有许多其它药物无法比拟的独特性质,以顺铂为代表的铂类抗癌药物在癌症临床化疗中发挥了巨大作用。但是铂类药物的毒副作用严重限制了它们的实际疗效和适用范围,因此需要继续研究具有不同作用机理的新型金属抗癌药物,以改良或补充现有铂类药物的性能。本文重点介绍了近年来设计金属抗癌药物的一些新策略,包括改变铂类药物与DNA的作用模式、改进铂类药物对肿瘤的靶向性、研发非铂类金属抗癌药物和寻找DNA以外的作用靶标等。这些内容体现了该领域的最新发展趋势,为从事金属抗癌药物开发研究的科技人员提供了有益的参考信息。Metal-based anticancer agents have many unique properties that are superior to those of other drugs. As a representative of platinum anticancer drugs, cisplatin plays a crucial role in the treatment of various cancers in clinical chemotherapy. However, the actual efficacy and applicability of this sort of drugs have been greatly limited by their severe toxic side-effects. In order to mend the defects of current platinum drugs, it is necessary to develop novel metalbased anticancer agents with different mechanism of action. In this review, some new strategies for the design of metalbased anticancer drugs are discussed. These include （1） altering the interaction mode of platinum drugs with DNA, （2） enhancing the tumor-targeting property of platinum drugs, （3） developing non-platinum metal-based anticancer drugs, and （4） exploring new potential biological targets other than DNA. All these respects reflect the major trends in this field, which provide some valuable information for researchers pursuing new metal-based anticancer agents.

关 键 词：金属配合物 抗癌药物 毒副反应 设计策略 

分 类 号：R914.3[医药卫生—药物化学] R979.1[医药卫生—药学]