Title:A Review on Acridines as Antiproliferative Agents
Volume: 22
Issue: 21
Author(s): Aparna Baliwada, Kalirajan Rajagopal*, Potlapati Varakumar, Kannan Raman and Gowramma Byran
Affiliation:
- Department of Pharmaceutical Chemistry, JSS College of Pharmacy (JSS Academy of Higher Education & Research)
Ooty, The Nilgiris, Tamil Nadu, India
Keywords:
Acridine, antiparasitic, anti-bacterial, antiviral, anti-tumor activity, DNA.
Abstract:
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.
Background: 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.
Objective: The objective of this study is to review the activity of acridines as anti-proliferative
agents.
Methods: 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.
Conclusion: 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.