Heterocyclic compounds containing imidazole moiety have shown therapeutic applications in diverse disease areas such as, anthelmintic, analgesic, anti-bacterial, anti-fungal, antiviral, antitubercular, anti-cancer etc. Thus, imidazole-based compounds are attractive targets in the design of novel chemical structures for the discovery of new drugs. In the current study, we have designed/synthesized a host of compounds bearing imidazole, by multi-component reaction using the corresponding aldehydes, amines/ammonium acetate and diketo compounds i.e. benzil and pyridil. These compounds were tested for antitumor activity on the National Cancer Institute's 60 human cancer cell lines panel. This panel is organized into nine subpanels representing diverse histologies: leukemia, melanoma, and cancers of lung, colon, kidney, ovary, breast, prostate, and central nervous system. The screening showed several compounds to be highly active against different cancer types, causing growth inhibition at micro- or nano-molar concentrations. To understand the mode of action of the displayed cytotoxicity, A549 cells were treated with four compounds in dose and time dependent manner. Also, in-vitro assays were performed to learn about the effect of these compounds on A549 cells for apoptosis, migration, anchorage independent growth and cellular senescence. Results of these investigations suggest cell migration and induced activation of caspase 3&9. Further studies for the cell cycle analysis and, to understand how intracellular signaling pathways that are known to be implicated in cancer progression might be altered by these compounds, are in progress.

Synthesis and investigation of the anticancer activity of imidazole-based new compounds

246th National Meeting (2013)

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