Department of Biochemistry, Institute of Chemistry, Faculty of Science, P. J. Šafárik University, Kosice, Slovak Republic.
Biomedical Research Center, University Hospital Hradec Kralove, Hradec Kralove, Czech Republic.
J Appl Toxicol. 2021 Jan;41(1):175-189. doi: 10.1002/jat.4072. Epub 2020 Sep 24.
Heterocycles have long been the focus of intensive study in attempts to develop novel therapeutic compounds, and acridine, a polynuclear nitrogen molecule containing a heterocycle, has attracted a considerable amount of scientific attention. Acridine derivatives have been studied in detail and have been found to possess multitarget properties, which inhibit topoisomerase enzymes that regulate topological changes in DNA and interfere with the essential biological function of DNA. This article describes some recent advancements in the field of new 9-substituted acridine heterocyclic agents and describes both the structure and the structure-activity relationship of the most promising molecules. The article will also present the IC values of the novel derivatives against various human cancer cell lines. The mini review also investigates the topoisomerase inhibition and antibacterial and antimalarial activity of these polycyclic aromatic derivatives.
杂环化合物一直是人们深入研究的焦点，试图开发新型治疗化合物，吖啶，一种含有杂环的多核氮分子，引起了相当多的科学关注。吖啶衍生物已被详细研究，发现具有多靶点特性，可抑制拓扑异构酶酶，调节 DNA 的拓扑变化，并干扰 DNA 的基本生物学功能。本文描述了新型 9-取代吖啶杂环试剂领域的一些最新进展，并描述了最有前途的分子的结构和构效关系。本文还将介绍新型衍生物对各种人癌细胞系的 IC 值。该小型综述还研究了这些多环芳烃衍生物的拓扑异构酶抑制、抗菌和抗疟活性。
