摘要
目的对DNA拓扑异构酶I(topoisomerase I,Topo I)抑制剂的种类,构效关系进行总结,以期对于研究DNA Topo I抑制剂药物提供参考。方法通过系统文献调研,以近年来50余篇文献为依据进行归纳总结。结果肿瘤细胞中DNA Topo I的表达过度,以DNA Topo I作为抗肿瘤药物的靶点非常有效,研究表明此类药物大多都具有较好的抗肿瘤活性。结论以研究DNA Topo I抑制剂作为抗肿瘤药物的研究方向具有很广阔的研究空间。
Objective To summarize the types of DNA topoisomeraseⅠinhibitors and the structure-activity relationship. Methods Based on the information from the literatures to sum up nearly all kinds of DNA topoisomerase Ⅰinhibitors. Results Investigation has indicated that this enzyme is over-expressive in various types of solid tumors,so it is prefect to use the topoⅠinhibitor for the treatment of cancer,meanwhile the structure modification of those compounds can improve its selectivity,therapeutic effect and reduce the side effect.Conclusion To study DNA Topo I inhibitors as anticancer drug has very broad space for the future research.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2015年第11期900-910,共11页
Journal of Shenyang Pharmaceutical University
基金
国家自然科学基金青年基金资助项目(No.81202425)
关键词
DNA拓扑异构酶抑制剂
抗肿瘤活性
构效关系
DNA topoisomeraseⅠinhibitors
antitumor activity
structure-activity relationship
