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.
キーワード
概要
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, as the mechanism of cell death, was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay.
RESULTS
Most of synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Apoptosis inducing of the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed by mentioned methods.
CONCLUSIONS
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.
