Novel VEGFR-2 inhibitors with an N-acylhydrazone scaffold.
Arch Pharm (Weinheim)
; 353(11): e2000130, 2020 Nov.
Article
em En
| MEDLINE
| ID: mdl-32667721
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neovascularização Fisiológica
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Inibidores da Angiogênese
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Receptor 2 de Fatores de Crescimento do Endotélio Vascular
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Membrana Corioalantoide
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Inibidores de Proteínas Quinases
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Hidrazonas
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article