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September 10, 2025European Journal of Medicinal ChemistryOpen Access

Examining the 2-aryl-5-nitrobenzofuran-based hydrazones for anti-breast (MCF-7) cancer activity, potential to induce cell cycle arrest and inhibit receptor tyrosine kinases (VEGFR-2 & EGFR)

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Authors

JNJackson K. NkoanaGMGarland K. MoreAEAhmed A. Elhenawy

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Overview

In vitro analysis demonstrated that hydrazones induce cell cycle arrest and inhibit EGFR and VEGFR-2, suggesting therapeutic potential.

Key Points

  • Compound 3k exhibited significant cytotoxicity against MCF-7 cells with an IC50 of 4.21 μM, indicating strong anti-breast cancer activity.
  • Cell cycle analysis revealed that compound 3k induced a G0/G1 phase arrest, with a 76.2% increase in early apoptosis observed.
  • Enzymatic assays confirmed potent VEGFR-2 inhibition by compound 2b (IC50 = 2.86 μM) and notable EGFR inhibition by compound 3f (IC50 = 5.29 μM).
  • Molecular modelling highlighted key structure-activity relationships, supporting the promising dual inhibition of VEGFR-2 and EGFR.

Cite This Study

Nkoana et al. (2025) studied this question.

synapsesocial.com/papers/68c2409bb210217d6479b250https://doi.org/10.1016/j.ejmech.2025.118018
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