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Novel VEGFR-2 inhibitors with an N-acylhydrazone scaffold
- Source :
- Archiv der PharmazieREFERENCES. 353(11)
- Publication Year :
- 2020
-
Abstract
- Vascular endothelial growth factor receptor 2 (VEGFR-2) is a tyrosine kinase that mediates a large number of cell responses associated with angiogenesis. The control of the angiogenic pathway in tumorigenesis by the inhibition of VEGFR-2 is considered a promising therapeutic strategy for the prevention and control of solid tumor growth. In this study, the design, synthesis, and biological evaluation of a novel series of VEGFR-2 inhibitors with an N-acylhydrazone (NAH) scaffold (9a-h) are reported. The molecular design is validated by docking studies and by in vitro inhibitory activity assays. Compounds 9b, 9c, 9d, and 9f effectively inhibited neovascularization induced by VEGF in the chorioallantoic membrane assay. Thus, these NAH derivatives are promising antiangiogenic prototypes.
- Subjects :
- Angiogenesis
Pharmaceutical Science
Neovascularization, Physiologic
Angiogenesis Inhibitors
Chick Embryo
01 natural sciences
Chorioallantoic Membrane
Neovascularization
Structure-Activity Relationship
Drug Discovery
medicine
Animals
Molecular Targeted Therapy
Protein Kinase Inhibitors
Molecular Structure
010405 organic chemistry
Chemistry
Hydrazones
Kinase insert domain receptor
Vascular Endothelial Growth Factor Receptor-2
In vitro
0104 chemical sciences
Angiogenesis inhibitor
Molecular Docking Simulation
010404 medicinal & biomolecular chemistry
Chorioallantoic membrane
Docking (molecular)
Drug Design
Cancer research
medicine.symptom
Tyrosine kinase
Subjects
Details
- ISSN :
- 15214184
- Volume :
- 353
- Issue :
- 11
- Database :
- OpenAIRE
- Journal :
- Archiv der PharmazieREFERENCES
- Accession number :
- edsair.doi.dedup.....02a414407462d8510eada0cab0a094eb