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Imidazole-pyridine hybrids as potent anti-cancer agents

Publication Type : Journal Article

Publisher : Elsevier

Source : European Journal of Pharmaceutical Sciences Volume 180 Pages 106323, 2023

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Campus : Coimbatore

School : School of Physical Sciences

Year : 2023

Abstract : In the current investigation, fifteen novel imidazole-pyridine-based molecules were synthesized and tested against cell lines of the lung (H1299) and colon (HCT116) adenocarcinomas by proliferation assay. The results demonstrated that compounds 5a, 5d, 5e, and 5f were the most active (IC50<30 µM). Based on recent literature and the current results, the glycogen synthase kinase-3β (GSK-3β) protein was investigated in-silico as a possible target. The molecular docking and QSAR revealed an excellent binding affinity of the selected imidazole-pyridine compounds to GSK-3β. Notably, GSK-3β protein levels were significantly upregulated in hepatocellular liver carcinoma (LIHCs) tissues and negatively affected patient prognosis. Consequently, the compounds were evaluated on liver cancer cell lines (HepG2, HUH-7, and PLC/PRF/5) by the MTT assay, and 5d showed the highest antitumor activity. This study offers new compounds with interesting biological activity on GSK-3β as a target, exhibiting a potential therapeutic impact for hepatocellular carcinoma patients.

Cite this Research Publication : Baladhandapani Aruchamy, Carmelo Drago, Venera Russo, Giovanni Mario Pitari, Prasanna Ramani, TP Aneesh, Sonu Benny, VR Vishnu, "Imidazole-pyridine hybrids as potent anti-cancer agents", European Journal of Pharmaceutical Sciences Volume 180 Pages 106323, 2023

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