Novel 1,2,5-Trisubstituted Benzimidazoles Potentiate Apoptosis by Mitochondrial Dysfunction in Panel of Cancer Cells

Jagadeesha, G. S. and Sudhanva, M. S. and Anil Kumar, B. M. and Akshay, Uttarkar and Shwetha, B. and Sridhar, B. T. and Vidya, N. and Shobith, R. and Rangappa, K. S. and Thimmegowda, N. R. (2022) Novel 1,2,5-Trisubstituted Benzimidazoles Potentiate Apoptosis by Mitochondrial Dysfunction in Panel of Cancer Cells. ACS Omega, 7 (50). 46955 – 46971. ISSN 24701343

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Abstract

Synthetic small molecules have been very effective in decimating cancer cells by targeting various aberrantly overexpressed oncogenic proteins. These small molecules target proteins involved in cell cycle regulation, cell division, migration, invasion, angiogenesis, and other regulatory proteins to induce apoptosis in cancer cells. In this study, we have synthesized a novel 1,2,5-trisubstituted benzimidazole chemical library of small molecules and unveiled their anticancer potential against a panel of cancer cell lines such as Jurkat, K-562, MOLT-4, HeLa, HCT116, and MIA PaCa-2 cancer cells. The MTT assay and Trypan blue dye exclusion assay clearly unveiled the cytotoxic effect of methyl 1-benzyl-2-(4-fluoro-3-nitrophenyl)-1H-benzodimidazole-5-carboxylate (TJ08) and its potential to induce apoptosis with effective IC50 of 1.88 ± 0.51, 1.89 ± 0.55, 2.05 ± 0.72, 2.11 ± 0.62, 3.04 ± 0.8, and 3.82 ± 0.25 μM against Jurkat, K562, MOLT-4, HeLa, HCT116, and MIA PaCa-2 cancer cell lines, respectively. Altered mitochondrial membrane potential was observed in HeLa, HCT116, and Jurkat cells due to TJ08 treatment, which was unveiled by JC10 staining. Induction of early and late apoptosis by TJ08 treatment was also unveiled by apoptotic analysis and immunofluorescence imaging. Cell cycle analysis distribution confirms the accumulation of cells in the S-phase in a dose-dependent manner. © 2022 American Chemical Society.

Item Type:	Article
Uncontrolled Keywords:	Alkyls, Anions, Apoptosis,Cells, Mixtures
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Institution of Excellence
Depositing User:	Manjunatha Library Assistant
Date Deposited:	01 Dec 2025 07:23
Last Modified:	01 Dec 2025 07:46
URI:	http://eprints.uni-mysore.ac.in/id/eprint/18125

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