Two series of novel imidazo[1,2-a]pyridine-2-carbohydrazide derivatives have been designed, synthesized and evaluated for cytotoxic activity. Target compounds were designed in two series: aryl hydrazone derivatives that were devoid of triazole moiety (7a-e) and aryl triazole group (11a-e). In vitro cytotoxicity screening was carried out using MTT assay against three human cancer cells including breast cancer (MCF-7), colon cancer (HT-29) and leukemia (K562) cell lines. Compound 7d bearing 4-bromophenyl pendant from aryl hyrazone series exhibited the highest cytotoxic potential with IC50 values of 22.6 µM and 13.4 µM against MCF-7 and HT-29 cells, respectively. Cell cycle analysis revealed that 7d decreased the cells in the G2/M phase at 50 and 100 µM concentrations. Overall, 7d could serve as a suitable candidate for further modifications as a lead anticancer structure.
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