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A comprehensive review on acridone based derivatives as future anti-cancer agents and their structure activity relationships

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 239, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2022.114527

Keywords

Acridone derivatives; Biological targets; DNA topoisomerase; Telomerase; P-gp; SAR

Funding

  1. DHR Project - Department of Health Research, Government of India [V. 25011/547-HRD/2016-HR]

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The clinical efficacy of existing anticancer drugs has been reduced due to drug resistance and severe side-effects. Therefore, the development of new anti-cancer drugs with minimal adverse effects is always needed. Acridone is a promising heterocycle that has gained attention for its ability to act on various molecular targets, overcome drug resistance, and intercalate DNA in cancer cells. Some acridone derivatives have already entered clinical studies and have shown great potential in cancer therapeutics and imaging.
The development of drug resistance and severe side-effects has reduced the clinical efficacy of the existing anticancer drugs available in the market. Thus, there is always a constant need to develop newer anti-cancer drugs with minimal adverse effects. Researchers all over the world have been focusing on various alternative strategies to discover novel, potent, and target specific molecules for cancer therapy. In this direction, several heterocyclic compounds are being explored but amongst them one promising heterocycle is acridone which has attracted the attention of medicinal chemists and gained huge biological importance as acridones are found to act on different therapeutically proven molecular targets, overcome ABC transporters mediated drug resistance and DNA intercalation in cancer cells. Some of these acridone derivatives have reached clinical studies as these heterocycles have shown huge potential in cancer therapeutics and imaging. Here, the authors have attempted to compile and make some recommendations of acridone based derivatives concerning their cancer biological targets and in vitro-cytotoxicity based on drug design and novelty to increase their therapeutic potential. This review also provides some important insights on the design, receptor targeting and future directions for the development of acridones as possible clinically effective anti-cancer agents.

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