Current drug targets · 2026
Quinazoline-based VEGFR-2 Inhibitors: A Comprehensive Review of Design Strategies, SAR, and Therapeutic Advances.
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Yadav Adarsh Kumar, Shah Drashti, Desai Princy, Kulkarni Utkarsha, Shah Ashish, Nagani Afzal, Patel Paresh, Patel Divy, Patel Ashish
Аннотация
INTRODUCTION: Angiogenesis, primarily controlled by Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2), significantly influences tumor growth and metastasis. Consequently, VEGFR-2 targeting has emerged as an important strategy for cancer treatment. Owing to their known efficacy as strong tyrosine kinase inhibitors, quinazoline-based heterocycles have attracted considerable interest in medicinal chemistry.
METHODS: The pharmacophoric properties, Structure-Activity Relationship (SAR) insights, and therapeutic advancements of quinazoline-based VEGFR-2 inhibitors documented in recent literature were thoroughly examined in this review.
RESULTS: By interacting with the DFG motif (Aspartate-Phenylalanine-Glycine) and forming hydrogen bonds with essential hinge residues like Cys919, Glu885, and Asp1046, quinazoline scaffolds effectively inhibit VEGFR-2. According to SAR studies, the quinazoline core is essential for increasing potency and selectivity when coupled with urea or amide bonds and electron-withdrawing substituents. Derivatives with better inhibitory activity have been produced through recent structural changes, such as halogen substitutions and fused heterocycles.
DISCUSSION AND CONCLUSION: Quinazolines serve as efficient scaffolds for occupying hydrophobic subpockets within the VEGFR-2 active site, as discussed. These results highlight the clinical importance of quinazoline derivatives and imply that the development of hybrid analogues in the future has enormous potential to advance targeted cancer treatments.
METHODS: The pharmacophoric properties, Structure-Activity Relationship (SAR) insights, and therapeutic advancements of quinazoline-based VEGFR-2 inhibitors documented in recent literature were thoroughly examined in this review.
RESULTS: By interacting with the DFG motif (Aspartate-Phenylalanine-Glycine) and forming hydrogen bonds with essential hinge residues like Cys919, Glu885, and Asp1046, quinazoline scaffolds effectively inhibit VEGFR-2. According to SAR studies, the quinazoline core is essential for increasing potency and selectivity when coupled with urea or amide bonds and electron-withdrawing substituents. Derivatives with better inhibitory activity have been produced through recent structural changes, such as halogen substitutions and fused heterocycles.
DISCUSSION AND CONCLUSION: Quinazolines serve as efficient scaffolds for occupying hydrophobic subpockets within the VEGFR-2 active site, as discussed. These results highlight the clinical importance of quinazoline derivatives and imply that the development of hybrid analogues in the future has enormous potential to advance targeted cancer treatments.