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This study aims to design and evaluate benzimidazole derivatives as inhibitors of VEGFR-2 for cancer therapy.

Benzimidazole‐Based VEGFR‐2 Inhibitors Inspired by Sorafenib: Synthesis, Biological Evaluation, and Mechanistic Insights

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Randomized trial investigates VEGFR-2 inhibition in cancer models, highlighting therapeutic potential.

This study aims to design and evaluate benzimidazole derivatives as inhibitors of VEGFR-2 for cancer therapy.
Twenty-six benzimidazole derivatives synthesized and evaluated for VEGFR-2 inhibition.
In vitro kinase assays conducted to assess inhibitory activity with IC50 values measured.
Mechanistic studies performed on selected compounds to analyze their effects on cell cycle and apoptosis.
The most active compound 3f showed IC50 values of 13.34 µM (HUVEC), 5.32 µM (MCF-7), and 5.02 µM (HepG2).
Compound 3f induced G2/M-phase cell cycle arrest and increased apoptosis in tested cell lines.
Evaluation against normal cell lines demonstrated good biocompatibility and selectivity.

Dewidar et al. (2026) studied this question.

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