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 and structure-activity relationships of topoisomerase I (Topo I) inhibitors in order to provide reference for the study of DNA Topo I inhibitors. Methods Through systematic literature research, based on more than 50 articles in recent years, the paper summarizes the results. Results DNA Topo I was overexpressed in tumor cells and DNA Topo I was very effective as a target of antitumor drugs. Studies have shown that most of these drugs have good antitumor activity. Conclusion There is a great research space to study DNA Topo I inhibitors as antineoplastic drugs.