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

[摘要] Objectives: In this study, some novel 2-(2-phenyl)-1H-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)-1H-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-GloTM 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.

[关键词] Benzimidazole;acetohydrazide;epidermal growth factor receptor kinase;inhibitory