A Review on Acridines as Antiproliferative Agents

Area of Science:

• Medicinal Chemistry
• Organic Chemistry
• Pharmacology

Background:

• Acridine derivatives possess multitarget properties with applications in medicine and industry.
• Research interest in acridines is growing due to their antibacterial, antimalarial, antiviral, and antitumor activities.
• Acridines interact with topoisomerase II and DNA base pairs, highlighting their potential as anti-tumor agents.

Purpose of the Study:

• To review the antiproliferative activity of acridine derivatives.
• To analyze the structure-activity relationships of novel 9-substituted acridine heterocyclic compounds.

Main Methods:

• Review of acridines as topoisomerase I and II inhibitors/poisons.
• Examination of acridines' interaction with G-quadruplex DNA.
• Analysis of acridines in metal complexes, quinacrine scaffolds, and with sulfur moieties.

Main Results:

• Novel 9-substituted acridine compounds exhibit promising antiproliferative activity against human cancer cell lines.
• Structure-activity relationship analyses reveal key molecular features for enhanced efficacy.
• IC50 values for new compounds against various cancer cell lines are presented.

Conclusions:

• Acridine derivatives remain scientifically relevant, offering diverse biological activities.
• Dominant mechanisms of action include DNA intercalation and enzyme inhibition.
• Further research into acridine derivatives holds potential for developing new therapeutic agents.