DNA拓扑异构酶酶广泛分布于所有生命领域中，对细胞功能至关重要。由于在DNA复制和转录过程中维护DNA拓扑结构的作用，许多抗菌和抗癌化疗药物靶向各种拓扑异构酶酶。源自天然产物，如蒽环类化合物、表莲二甲氧苯丙烷和喹诺酮衍生物的药物已广泛用于治疗各种癌症。有一个非常活跃的基础和临床研究领域是针对拓扑异构酶II酶的选择性靶向治疗癌症。本主题评述总结了最有效的拓扑异构酶II抑制剂（蒽环类化合物、表莲二甲氧苯丙烷和氟喹诺酮类）在过去的十年（从2013年到2023年）中的抗癌活性、作用方式和结构活性关系（SARs），并按时间顺序组织。该综述还强调了有前途的新型拓扑异构酶II抑制剂的作用机制和SARs。版权所有 © 2023 Elsevier Inc.

The DNA topoisomerase enzymes are widely distributed throughout all spheres of life and are necessary for cell function. Numerous antibacterial and cancer chemotherapeutic drugs target the various topoisomerase enzymes because of their roles in maintaining DNA topology during DNA replication and transcription. Agents derived from natural products, like anthracyclines, epipodophyllotoxins and quinolones, have been widely used to treat a variety of cancers. A very active field of fundamental and clinical research is the selective targeting of topoisomerase II enzymes for cancer treatment. This thematic review summarizes the recent advances in the anticancer activity of the most potent topoisomerase II inhibitors (anthracyclines, epipodophyllotoxins and fluoroquinolones) their modes of action, and structure-activity relationships (SARs) organized chronologically in the last ten years from 2013 to 2023. The review also highlights the mechanism of action and SARs of promising new topoisomerase II inhibitors.Copyright © 2023 Elsevier Inc. All rights reserved.