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Herein, we described the synthesis of some new aromatic amides of 4β‐imidazolopodophyllotoxin (6 a–p) and their anticancer evaluation against four human cancer cell lines like MCF‐7 (breast), A549 (lung), Hela (cervical) and DU‐145 (prostate). Out of all, compounds 6 d, 6 e, 6 g, 6 i, 6 j, 6 l, 6 n and 6 o were found to be active with IC50 values in the range of 0.59‐10 μM. Specifically, compound 6 o showed greater potency against all the cell lines than the standard etoposide. Predominantly, compounds 6 e, 6 j and 6 o observed to be 3 to 4 times more potent against DU‐145 than the standard. The molecular docking studies of three active compounds 6 e, 6 j and 6 o on target protein DNA topoisomerase II were also conducted and found that binding affinity and free energies obtained were in good covenant with the corresponding IC50 values. Finally, the results of in silico ADMET revealed that, compounds 6 e, 6 j and 6 o have shown 100 % intestinal absorption and none of them exhibited AMES and hepato toxicity. [ABSTRACT FROM AUTHOR]