Novel fused pyran derivatives induce apoptosis and target cell cycle progression in anticancer efficacy against multiple cell lines

Nitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives ( 6a-e , 8a-e , 10a-e , 12a-e , & 14a-e ) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer...

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Bibliographic Details
Published in:New journal of chemistry 2024-05, Vol.48 (18), p.838-854
Main Authors: Fabitha, K, Kallingal, Anoop, Maciejewska, Natalia, Arya, C. G, Chandrakanth, Munugala, Thomas, Neethu Mariam, Li, Yupeng, Gondru, Ramesh, Munikumar, Manne, Banothu, Janardhan
Format: Article
Language:English
Subjects:
Anticancer properties
Apoptosis
Benzotriazole
Cancer
Cell cycle
Damage assessment
Imidazole
Pyrazole
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Summary:Nitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives ( 6a-e , 8a-e , 10a-e , 12a-e , & 14a-e ) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines. Among the compounds, 6e , 14b , and 8c were identified as the most potent against MCF7, A549, and HCT116, with IC 50 values of 12.46 ± 2.72 μM, 0.23 ± 0.12 μM, and 7.58 ± 1.01 μM, respectively. Further studies demonstrated that these compounds can change cellular and nuclear morphology and inhibit colony formation in the tested cancer cells. They also remarkably block/inhibit the cell cycle progression of cancer cells at various phases. DNA damage analysis and apoptosis studies revealed that these compounds have the potential to induce DNA double-strand breaks and apoptosis. In silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the potent compounds were assessed, revealing that all the compounds exhibited favorable pharmacokinetic and toxicological properties. The potent compounds identified from this study can be considered as a lead for further drug design and development. Nitrogen-based heterocycles substituted fused pyran derivatives ( 6a-e , 8a-e , 10a-e , 12a-e , & 14a-e ) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines.
ISSN:1144-0546
1369-9261
DOI:10.1039/d4nj00824c