Background: Benzimidazole derivatives are privileged molecules known with wide variety of biological
activity. In medicinal chemistry, due to the ring’s structural similarity to nucleotides its derivatives were investigated
as new chemotheraupeutic agents. Our research group have been studying about 1,2-disubstituted benzimidazoles
including thiocarbamoyl group and their potential anticancer activity. Based on previous findings, we have
synthesized novel 1-[2-(4-substituted phenyl-2-oxoethyl)]-2-[(2/3/4-substituted phenylpiperidin-1-
yl)thiocarbamoyl]benzimidazole derivatives (3a-o).
Methods: The obtained fifteen derivatives were studied on A549 adenocarcinomic human alveolar basal epithelial
cell line and mouse L929 fibroblastic cell line to determine their cytotoxic activity. These compounds were also
investigated to identify their apoptotic properties.
Results: The structures of the compounds based on three different groups, they differ from each other with the
phenyl substituents bonded to piperazine ring. All of the compounds showed remarkable antitumor activity, but first
five compounds bearing non-substituted phenyl moiety exhibited selective cytotoxicity when compared potencies
to normal cell line.
Conclusion: Compounds 3j, 3m and 3n were identified as the most apoptotic derivatives, however compounds 3e
and 3h provoked apoptosis with the percentages of 10.6 and 10.9 % and selective cytotoxicity.