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
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.