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Recent progress of small molecular VEGFR inhibitors as anticancer agents

D Xu1, T-L Wang, L-P Sun

  • 1Department of Medicinal Chemistry, China Pharmaceutical University, No. 24, Tongjiaxiang Rd, Nanjing, 210009, Jiangsu Province, P.R. China.

Mini Reviews in Medicinal Chemistry
|November 2, 2010
PubMed

Insights

Small molecule inhibitors targeting vascular endothelial growth factor receptor (VEGFR) are crucial for cancer treatment. This review details their development, structure, and clinical progress, focusing on market-available and advanced-stage compounds.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Vascular endothelial growth factor receptor (VEGFR) is a key receptor tyrosine kinase (RTK) regulating angiogenesis.
  • Aberrant VEGFR signaling is implicated in various diseases, notably cancer.

Purpose of the Study:

  • To review the progress in the design and synthesis of small molecular VEGFR inhibitors for cancer research.
  • To highlight compounds in clinical trials and on the market.

Main Methods:

  • Literature review of recent advancements in VEGFR inhibitor development.
  • Analysis of structural and pharmacophore features.
  • Evaluation of biological activities and structure-activity relationships (SAR).

Main Results:

  • Significant progress in developing small molecule VEGFR inhibitors.
  • Detailed insights into the structure, activity, and SAR of these inhibitors.
  • Identification of compounds with clinical relevance.

Conclusions:

  • VEGFR kinase inhibition is a vital strategy in cancer therapy.
  • Ongoing research continues to yield promising inhibitors for clinical application.

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