Synthesis and antitumor activity of 1-substituted-2-methyl-5-nitrobenzimidazoles

Different substituents were introduced in position 1 of 2-methyl-5(6)-nitro-1H-benzimidazole (2) in order to obtain different side chains having different heterocyclic compounds, for example, thiadiazoles (5–7), tetrazoles (8, 9a, b), triazoles (11–13), thiazoles (14a–e), triazines (10, 16, 17), and imidazoles (18a–c). The antitumor effect of compounds 1, 2, 2a, 4, 5, 7, 8, 9a, 10, 13, 14a, 15, 16, and 18c was studied against breast cancer (MCF7) and compounds 2 [IC50 = 4.52 μg] and 7 [IC50 = 8.29 μg] were found to be active.

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