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A Simple Bioassay for the Evaluation of Vascular Endothelial Growth Factors
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Structure-activity relationship studies of indolin-2-one derivatives as vascular endothelial growth factor receptor

Mozhdeh Yousefian1,2, Razieh Ghodsi1,2

  • 1Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.

Archiv Der Pharmazie
|September 5, 2020
PubMed

Insights

Novel indolin-2-one compounds targeting vascular endothelial growth factor receptors (VEGFRs) show promise for cancer treatment. Modifications to the indolin-2-one scaffold, particularly at the C-3 position, are key to enhancing antiangiogenic and anticancer effects.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Oncology

Background:

  • Angiogenesis is crucial for cancer cell proliferation and metastasis.
  • Vascular Endothelial Growth Factor Receptors (VEGFRs) are key targets for anti-cancer therapies.
  • Indolin-2-one derivatives, like Sunitinib, are established VEGFR inhibitors used in cancer treatment.

Purpose of the Study:

  • To review the structure-activity relationships of indolin-2-one analogs as VEGFR inhibitors.
  • To explore novel indolin-2-one compounds designed to improve upon Sunitinib's efficacy and safety.
  • To understand how modifications to the indolin-2-one scaffold impact antiangiogenic and anticancer activities.

Main Methods:

  • Comprehensive literature review of indolin-2-one derivatives as VEGFR inhibitors.
  • Analysis of structure-activity relationships (SAR) based on published studies.
  • Discussion of synthetic strategies and biological evaluation of novel analogs.

Main Results:

  • The indolin-2-one core is essential for VEGFR inhibition.
  • Substitutions at the C-3 position of the oxindole ring significantly influence antiangiogenic and anticancer potency.
  • Various analogs demonstrate improved anticancer activity, bioavailability, and solubility compared to Sunitinib.

Conclusions:

  • Indolin-2-one derivatives represent a promising class of antiangiogenic agents for cancer therapy.
  • Strategic modifications of the indolin-2-one scaffold, especially at C-3, can optimize anti-cancer drug profiles.
  • Further research into these analogs holds potential for developing more effective and safer cancer treatments.
Keywords:
VEGFRsangiogenesisanticancerindolin-2-onessunitinib

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