Discovery of 1H-benzo[d]imidazole-(halogenated) Benzylidenebenzohydrazide Hybrids as Potential Multi-Kinase Inhibitors.

ABSTRACT: In an effort to develop improved and effective targeted tyrosine kinase inhibitors (TKIs), a series of twelve novel compounds with the structural motif "(E)-4-(((1H-benzo[d]imidazol-2-yl)methyl)amino)-N'-(halogenated)benzylidenebenzohydrazide" were successfully synthesized in three steps, yielding high product yields (53-97%). Among this new class of compounds, 6c and 6h-j exhibited excellent cytotoxic effects against four different cancer cell lines, with half-maximal inhibitory concentration (IC₅₀) values ranging from 7.82 to 21.48 μM. Notably, compounds 6h and 6i emerged as the most potent inhibitors, demonstrating significant activity against key kinases such as EGFR, HER2, and CDK2. Furthermore, compound 6h disp

SUBMITTER: Mirgany TO 

PROVIDER: S-EPMC11279404 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature