Sulfonamides a Promising Hit for Cancer Therapy Through VEGFR-2 Inhibition

Eleftherios Charissopoulos1, Eleni Pontiki1

  • 1Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.

Biomedicines
|April 29, 2025
PubMed

Insights

Novel sulfonamide derivatives show promise as multi-target drugs for cancer therapy, inhibiting Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) and potentially overcoming resistance and side effects associated with current treatments.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Oncology

Background:

  • Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key target in anti-angiogenic cancer therapy due to its role in tumor angiogenesis.
  • Current VEGFR-2 inhibitors face challenges including drug resistance and cardiac side effects.
  • Developing novel therapeutic strategies is crucial to enhance efficacy and minimize adverse events.

Purpose of the Study:

  • To review novel compounds with potential VEGFR-2 inhibitory activity.
  • To explore multifunctional drugs targeting multiple pathways for improved cancer treatment.
  • To highlight sulfonamide derivatives as promising candidates in drug discovery.

Main Methods:

  • Literature review of recent studies on VEGFR-2 inhibitors.
  • Focus on sulfonamide derivatives with dual inhibitory activities.
  • Analysis of compounds targeting VEGFR-2 and carbonic anhydrase.

Main Results:

  • Identification of novel compounds with potential VEGFR-2 inhibitory activity.
  • Four compounds demonstrated additional carbonic anhydrase inhibitory activity.
  • Sulfonamide derivatives offer a versatile scaffold for developing multi-target agents.

Conclusions:

  • Novel sulfonamide derivatives represent a promising avenue for developing next-generation anti-angiogenic cancer therapies.
  • Multifunctional agents targeting VEGFR-2 and other pathways may overcome resistance and reduce side effects.
  • Further research into these compounds could lead to more effective cancer treatments.

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