2. Academic Validation
  3. Amino acid-modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer

Amino acid-modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer

  • Eur J Med Chem. 2025 Nov 5:297:117963. doi: 10.1016/j.ejmech.2025.117963.
Radwan El-Haggar 1,  Reem I Alsantali 2,  Ahmed M Aboshanab 3,  Mahmoud A Alkabbani 4,  Yara E Mansour 5,  Samar S Fatahala 5,  Nicolas Masurier 6
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt. Electronic address: radwan_elhaggar@pharm.helwan.edu.eg.
  • 2 Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O.Box 11099, Taif, 21944, Saudi Arabia.
  • 3 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt.
  • 4 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Egyptian Russian University, Cairo, 11829, Egypt.
  • 5 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt.
  • 6 Institut des Biomolécules Max Mousseron (IBMM), UMR 5247, CNRS, Université de Montpellier, ENSCM, Montpellier, France. Electronic address: nicolas.masurier@umontpellier.fr.
PMID: 40695035 DOI: 10.1016/j.ejmech.2025.117963
Abstract

A novel series of chalcone derivatives was developed with potent Anticancer activity against colon Cancer. Sixteen amino acid-based compounds, incorporating phenylalanine or tryptophan to improve aqueous solubility, were evaluated by the NCI on its 60-cell line panel. Eleven showed notable growth inhibition potencies, with five exhibiting high activity, particularly against the HCT116 colon Cancer cell line, and no significant toxicity on WI-38 fibroblasts. Compounds 5f and 5g were selected for further evaluation; both induced SubG0-G1 cell cycle arrest, secondary necrosis, and upregulation of Caspase-3, p53, and Bax/Bcl-2. Kinome inhibition profiling across 340 human kinases revealed that these compounds may act as PKC inhibitors, making them the first Chalcones reported with such activity. In vivo, both compounds significantly reduced tumor growth, with efficacy comparable to doxorubicin. These results highlight these compounds as promising candidates for further development as Anticancer agents, particularly for colon Cancer treatment.

Keywords

Amino-acid; Chalcone; Colon cancer; Necrosis; PKC inhibitors.

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