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2000
Volume 21, Issue 3
  • ISSN: 1573-4080
  • E-ISSN: 1875-6662

Abstract

Introduction

Xanthones, also known as dibenzo-γ-pyrone or 9H-xanthen-9-ones, constitute an essential group of oxygenated heterocycles that possess a dibenzo-pyrone structure having the chemical formula CHO. These compounds have generated significant interest due to their high taxonomic relevance and pharmacological characteristics. Xanthone and its derivatives are cytotoxic medications due to their planar structure and capacity to intercalate with Deoxyribonucleic acid (DNA). As a DNA intercalator, xanthone extraction and synthesis have become popular in cytotoxic research.

Methods

We developed a series of novel xanthone derivatives conventional synthesis and we then assessed their anticancer efficacy against the A549 human lung cancer cell line utilizing the MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. Furthermore, we conducted a docking study using a receptor with the Protein Data Bank (PDB) ID: IZXM to validate the anticancer activity of the synthesized compounds

Results

Drug likeliness and molecular docking studies confirmed the biopotential and anticancer effectiveness of novel human DNA topoisomerase IIα inhibitors. Our anticancer activity results indicated that synthesized compound 5a had the lowest half-maximal inhibitory concentration (IC) value and a higher cytotoxicity activity.

Discussion

The newly synthesized xanthone derivatives showed promising anticancer potential, particularly compound 5a, which exhibited favorable properties.

Conclusion

The study concluded that synthesizing new xanthone derivatives and evaluating their cytotoxic activity showed promising potency in compound 5a as an anticancer candidate. The synthesized compounds have silico drug-relevant properties, which ensure their potential leads for future drug discovery studies.

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Design, Synthesis and Preliminary Assessment of Novel Cytotoxic Xanthone-Based Derivatives Targeting Human DNA Topoisomerase IIα
Curr. Enzym. Inhib. 21, 209 (2025); https://doi.org/10.2174/0115734080339546250325164642
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  • Article Type:     Research Article
Keyword(s): amine based xanthone derivatives; cytotoxicity; dibenzo-γ-pyrone; in-silico; MTT assay; topoisomerase II; Xanthone

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