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A new look at 9-substituted acridines with various biological activities.
Journal of Applied Toxicology ( IF 2.7 ) Pub Date : 2020-09-24 , DOI: 10.1002/jat.4072
Maria Kozurkova 1, 2 , Danica Sabolova 1 , Pavol Kristian 3
Affiliation  

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 IC50 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.

中文翻译:

对具有各种生物活性的 9-取代吖啶的新看法。

长期以来,杂环一直是试图开发新型治疗化合物的深入研究的重点,而吖啶,一种含有杂环的多核氮分子,已引起了相当多的科学关注。已经详细研究了吖啶衍生物,并发现它具有多靶点特性,可抑制调节 DNA 拓扑变化的拓扑异构酶并干扰 DNA 的基本生物学功能。本文描述了新的 9-取代吖啶杂环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 IC 50新型衍生物对各种人类癌细胞系的价值。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作用以及抗菌和抗疟活性。
更新日期:2020-12-01
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