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Recent progress in the exploitation of anti-cancer small molecules targeting angiogenesis

Ying Zheng1, Hao Qiu1, Ke Zhang1

  • 1College of Traditional Chinese Medicine and Pharmacy, Clinical Medical Research Center, Affiliated Hospital of Jinggangshan University, Jiangxi Province Key Laboratory of Organ Development and Epigenetics, Jinggangshan University, Ji'an, China.

Journal of Enzyme Inhibition and Medicinal Chemistry
|November 20, 2025
PubMed

Insights

Novel small molecule angiogenesis inhibitors show significant efficacy in combating cancer by suppressing tumor growth and metastasis. This review details their design and structure-activity relationships, guiding future anti-cancer drug development.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Angiogenesis, the formation of new blood vessels, is essential for tumor growth and metastasis.
  • Antiangiogenic therapies target tumor vasculature, representing a key cancer treatment strategy.
  • Recent advancements have significantly improved antiangiogenic cancer therapies.

Purpose of the Study:

  • To comprehensively review small molecule angiogenesis inhibitors developed between 2014 and 2025.
  • To analyze the design, structure-activity relationships (SAR), and mechanisms of action of these inhibitors.
  • To provide insights for the development of next-generation anti-angiogenic cancer agents.

Main Methods:

  • Systematic literature review of small molecule angiogenesis inhibitors (2014-2025).
  • Analysis of drug design, SAR, and mechanisms of action.
  • Integration of the latest research findings in the field.

Main Results:

  • Numerous novel angiogenesis inhibitors demonstrate significant efficacy.
  • These inhibitors suppress angiogenesis, metastasis, and induce cancer cell apoptosis through various mechanisms.
  • Key advancements in small molecule inhibitor design and SAR have been identified.

Conclusions:

  • Small molecule angiogenesis inhibitors are a promising therapeutic strategy for cancer treatment.
  • Understanding their SAR and mechanisms is crucial for optimizing future drug development.
  • This review offers valuable insights for advancing next-generation anti-angiogenic therapies.
Keywords:
Anti-cancerFGFRHDACVEGFR-2angiogenesis

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