Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

Author(s): Faeze Khalili, Sara Akrami, Malihe Safavi, Maryam Mohammadi-Khanaposhtani, Mina Saeedi, Sussan K. Ardestani, Bagher Larijani, Afsaneh Zonouzi*, Maliheh B. Tehrani*, Mohammad Mahdavi*.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 19 , Issue 2 , 2019

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Graphical Abstract:


Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives.

Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated.

Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death.

Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods.

Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

Keywords: Anti-cancer, apoptosis, cytotoxicity, styrylimidazo[1, 2-a]pyridines, TUNEL assay, anti-breast cancer.

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Article Details

Year: 2019
Page: [265 - 275]
Pages: 11
DOI: 10.2174/1871520618666180903100835
Price: $58

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