<p>In this paper, a series of new 1,2,3-triazole-benzimidazoles hybrid structures, may exhibit potent anticancer activities, were designed and synthesized. The synthesis of the 1,2,3-triazole-benzimidazoles began with the preparation of 1,2,3-triazoles containing formyl precursors and then reacted with <i>o</i>-phenylenediamine to give 1,2,3-triazole-benzimidazole hybrid structures. 1,2,3-Triazole-benzimidazole complexes were tested for in vitro inhibition against human cancer cell lines such as breast (MCF-7) and colon (HCT116) by MTT assay. In particular, methyl 5-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-1-(3-chlorobenzyl)-1<i>H</i>-1,2,3-triazole-4-carboxylate and methyl 5-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-1-(2-methoxybenzyl)-1<i>H</i>-1,2,3-triazole-4-carboxylate showed the best activity in the MCF-7 line with IC₅₀ values of 52.15 and 42.96&#xa0;μg/cm³, respectively. For the HCT116 line, methyl 5-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-1-(3-chlorobenzyl)-1<i>H</i>-1,2,3-triazole-4-carboxylate and methyl 5-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-1-(4-chlorobenzyl)-1<i>H</i>-1,2,3-triazole-4-carboxylate showed the highest activity with IC₅₀ values of 15.89&#xa0;μg/cm³ and 18.89&#xa0;μg/cm³, respectively. In summary, the results of this study show that methyl 5-(1<i>H</i>-benzo-[<i>d</i>]imidazol-2-yl)-1-(3-chlorobenzyl)-1<i>H</i>-1,2,3-triazole-4-carboxylate with further modifications could serve as a leading drug candidate in future cancer studies in both MCF-7 and HCT116 strains.</p> Graphical abstract <p></p>