Synthesis, characterization and in vivo biological evaluation of novel benzimidazoles as potential anticancer agents

Objective: Cancer is one of the major cause of death worldwide irrespective of the sex. The aim of the study is to design, synthesize and identification of novel anti-proliferative agents that can potently target cancer. Methodology: We are reporting the synthesis of new series of N-substituted 2-(2-butyl-4-chloro-1 H -imidazole-5-yl)-1 H -benzo[d]imidazole derivatives and evaluated for their anti-tumor activity against HeLa cell lines. We identified the lead compound in the series and tested its anti-proliferative and anti-angiogenic properties against EAT bearing mice. Results: We identified 2-(2-butyl-4-chloro-1-heptyl-1H-imidazol-5yl)-1H-benzo[d]imidazole as a lead compound with the IC 50 of 25.3 µM. The lead compound is significantly decreases angiogenesis in peritoneum of EAT bearing mice. Conclusion: Our results clearly demonstrates that benzimidazoles suppresses the cell proliferation, peritoneal angiogenesis and ascites volume.