2020/01/01 by Kamila Buzun, Anna Bielawska, Krzysztof Bielawski +1 · 1 citation
Biochemistry, Genetics and Molecular Biology · Pharmacology, Toxicology and Pharmaceutics · Chemistry · #Cancer therapeutics and mechanisms #Bioactive Compounds and Antitumor Agents #Synthesis and biological activity
paper · pdf · doi:10.1080/14756366.2020.1821676
openalex publication_date 2020/01/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/29
The significant role of topoisomerases in the control of DNA chain topology has been confirmed in numerous research conducted worldwide. The prevalence of these enzymes, as well as the key importance of topoisomerase in the proper functioning of cells, have made them the target of many scientific studies conducted all over the world. This article is a comprehensive review of knowledge about topoisomerases and their inhibitors collected over the years. Studies on the structure-activity relationship and molecular docking are one of the key elements driving drug development. In addition to information on molecular targets, this article contains details on the structure-activity relationship of described classes of compounds. Moreover, the work also includes details about the structure of the compounds that drive the mode of action of topoisomerase inhibitors. Finally, selected topoisomerases inhibitors at the stage of clinical trials and their potential application in the chemotherapy of various cancers are described.