Monatshefte fur Chemie, cilt.156, sa.11, ss.1217-1226, 2025 (SCI-Expanded)
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 o-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-(1H-benzo[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate and methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(2-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate showed the best activity in the MCF-7 line with IC50 values of 52.15 and 42.96 μg/cm3, respectively. For the HCT116 line, methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate and methyl 5-(1H-benzo[d]imidazol-2-yl)-1-(4-chlorobenzyl)-1H-1,2,3-triazole-4-carboxylate showed the highest activity with IC50 values of 15.89 μg/cm3 and 18.89 μg/cm3, respectively. In summary, the results of this study show that methyl 5-(1H-benzo-[d]imidazol-2-yl)-1-(3-chlorobenzyl)-1H-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.