Synthesis and Pharmacologic Evaluation of Some Benzimidazole Acetohydrazide Derivatives as EGFR Inhibitors
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Updated: Dec 20, 2025
Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Serkan Demirel1, Gülgün Ayhan Kilcigil1, Zümra Kara2
1Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
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.
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