吖啶衍生物已被彻底研究和发现具有多目标质量,抑制调节DNA拓扑变化并干扰DNA重要生物学功能的拓扑异构酶。本文讨论了新型9-取代吖啶杂环化合物领域的最新进展,包括最有前途的分子的结构和结构-活性连接。新化合物对几种人癌细胞系的IC50值也将在该出版物中呈现。该综述还探讨了多环芳香化合物对拓扑异构酶的抑制作用。
吖啶环可以在许多不同领域使用的分子中找到,包括工业和医药。如今,由于细菌抗性降低,具有抗菌活性的吖啶具有研究兴趣。一些吖啶衍生物显示抗疟或抗病毒活性。由于与拓扑异构酶II和DNA碱基对的相互作用,还研究了吖啶衍生物的抗肿瘤活性。考虑到吖啶衍生物的这些可能的用途,这项工作概述了这些化合物的特定作用的所有重要结构性能。
本研究的目的是综述吖啶作为抗增殖剂的活性。
这篇综述被设计为吖啶作为拓扑异构酶I和II抑制剂/毒药,G-quadraplux相互作用上的cridines,吖啶与金属配合物,带有奎纳克林支架的acridines,带有硫部分的吖啶。
虽然在19世纪引入,吖啶衍生物仍然具有科学意义。在这次审查中,具有各种生物活性的吖啶衍生物(抗寄生虫,抗病毒,抗菌,和抗增殖)及其结构-活性关系分析。尽管已知它们的几种作用机制,唯一重要的是在这里讨论。可以得出结论,主要机制是DNA嵌入和与酶的相互作用。
Acridine derivatives have been thoroughly investigated and discovered to have multitarget qualities, inhibiting topoisomerase enzymes that regulate topological changes in DNA and interfering with DNA\'s vital biological function. This article discusses current progress in the realm of novel 9-substituted acridine heterocyclic compounds, including the structure and structure- activity connection of the most promising molecules. The IC50 values of the new compounds against several human cancer cell lines will also be presented in the publication. The
review also looks into the inhibition of topoisomerase by polycyclic aromatic compounds.
Acridine rings can be found in molecules used in many different areas, including industry and medicine. Nowadays, acridines with anti-bacterial activity are of research interest due to decreasing bacterial resistance. Some acridine derivatives showed antimalarial or antiviral activity. Acridine derivatives were also investigated for anti-tumor activity due to the interaction with topoisomerase II and DNA base pairs. Considering these possible uses of acridine derivatives, this work overviewed all significant structure performances for the specific action of these compounds.
The objective of this study is to
review the activity of acridines as anti-proliferative agents.
This
review is designed as acridines acting as topoisomerase I and II inhibitors/ poison, Acridines on the G-quadraplux interaction, Acridines with metal complexes, Acridines with quinacrine scaffold, Acridines with sulphur moiety.
Although introduced in the 19th century, acridine derivatives are still of scientific interest. In this
review, acridine derivatives with various biological activities (antiparasitic, antiviral, anti-bacterial, and antiproliferative) and their structure-activity relationship analyses are presented. Although several mechanisms of their action are known, the only important are discussed here. It can be concluded that the dominant mechanisms are DNA intercalation and interaction with enzymes.