Synthesis and Pharmacologic Evaluation of Some Benzimidazole Acetohydrazide Derivatives as EGFR Inhibitors.

Objectives: In this study, some novel 2-(2-phenyl)-1-benzo[d]imidazol-1-yl)-N'-(arylmethylene) acetohydrazide derivatives (1-12) were designed and synthesized.

Materials And Methods: Compounds 1-12 were obtained by condensing 2-(2-phenyl)-1-benzo[d]imidazol-1-yl)acetohydrazide (III) with the corresponding aromatic aldehyde derivatives in the presence of catalytic amounts of hydrochloric acid in ethanol.

Results: Following the structure elucidation, epidermal growth factor receptor kinase inhibitor activity was measured. The ADP-Glo kinase assay determines kinase activity based on the quantification of the amount of ADP produced during a kinase reaction.

Conclusion: Almost all of the compounds' kinase inhibitor activities were rather limited.