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Advances in Quinazolinone-Based Tumor-Targeted Inhibitors
Jieming Li1,2, Shuaiyi Lv1,2, Bin Yang3
1Henan University of Chinese Medicine, Zhengzhou, China.
Chemistry & Biodiversity
|June 11, 2026
Summary
Quinazolinone derivatives show promise as targeted antitumor agents by inhibiting key cancer pathways like tyrosine kinases (EGFR, VEGFR). Novel compounds offer dual-target synergy to combat tumor heterogeneity and drug resistance.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Oncology
Background:
- Quinazolinone derivatives possess a versatile scaffold for developing targeted antitumor agents.
- Their structural tunability allows for optimization of pharmacological properties.
Purpose of the Study:
- To systematically review recent advancements in the antitumor pharmacology of quinazolinone derivatives.
- To summarize their multifaceted mechanisms of action and target inhibitor development.
Main Methods:
- Literature review of preclinical and clinical studies on quinazolinone derivatives.
- Analysis of structure-activity relationships (SAR) for optimized drug design.
Main Results:
- Quinazolinones effectively inhibit tyrosine kinases (e.g., EGFR, VEGFR), PI3K/AKT/mTOR signaling, and epigenetic regulators.
- These mechanisms block tumor proliferation, induce apoptosis, and reduce angiogenesis and metabolic reprogramming.
- Novel derivatives demonstrate dual-target synergy, overcoming resistance and addressing tumor heterogeneity.
Conclusions:
- Quinazolinone derivatives represent a promising class of targeted antitumor agents with diverse mechanisms.
- SAR studies and dual-target strategies are crucial for developing effective cancer therapies.
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