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

Serkan Demirel; Gülgün Ayhan Kilcigil; Zümra Kara; Berna Güven; Arzu Onay Beşikci

doi:10.4274/tjps.24008

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

Turk J Pharm Sci. 2017 Dec;14(3):285-289. doi: 10.4274/tjps.24008. Epub 2017 Nov 20.

Authors

Serkan Demirel¹, Gülgün Ayhan Kilcigil¹, Zümra Kara², Berna Güven², Arzu Onay Beşikci²

Affiliations

¹ Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
² Ankara University, Faculty of Pharmacy, Department of Pharmacology, Ankara, Turkey.

Abstract

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-Glo^TM 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.

Keywords: Benzimidazole; acetohydrazide; epidermal growth factor receptor kinase; inhibitory.