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DNA拓扑异构酶Ⅰ(topoisomeraseⅠ,TopoⅠ)参与DNA的复制、转录、重组和修复等所有关键的核过程。近几年,其抗肿瘤小分子抑制剂的研究逐渐成为热点。该文对21世纪以来报道的新拓扑异构酶Ⅰ天然产物抑制剂的结构、生物活性及结构改造等进行系统的综述,以期为设计全新结构的拓扑异构酶Ⅰ抑制剂提供指导。
Topoisomerase Ⅰ (TopoⅠ) participates in all key nuclear processes such as DNA replication, transcription, recombination and repair. In recent years, its anti-tumor small molecule inhibitors research has gradually become a hot spot. This review summarizes the structure, biological activity and structural modification of novel topoisomerase I natural product inhibitors reported since the 21st century in order to provide guidance for the design of novel topoisomerase I inhibitors.