A series of 2-heteroaryl benzimidazole-chalcone hybrids were synthesized and the anticancer
activity was estimated by MTT assay in human breast, lung, colon, and ovarian cancer cell lines. The
biological results indicate that the compounds showed good anticancer activity with IC50 value in the
range of 0.056-19.5 μM. Compound 11b with hexa methoxy groups, bearing three methoxy groups on
each terminal aryl ring exhibited a significant IC50 value (56 nM) against human breast carcinoma cells,
which is 37 times higher potency in comparison with the reference Etoposide. Further compounds substituted
variably with methoxy and nitro groups on the phenyl ring of chalcone showed more promising
anticancer activity than the compounds with unsubstituted phenyl ring or variably alkyl-substituted phenyl
ring of chalcone. The molecular docking results indicate that the synthesized compounds bind in the
active site of Abl tyrosine kinase, the target of anticancer drug Imatinib. The present study provides the
synergistic effect of hybrids, benzimidazole-chalcones as potential anticancer agents that will aid in the
discovery of new anticancer agents.
Keywords: Chalcones, benzimidazoles, hybrids, anticancer activity, licochalcone A, nocodazole, Abl tyrosine kinase, imatinib.
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