Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2.
Future Med Chem
; 13(22): 1963-1986, 2021 11.
Article
em En
| MEDLINE
| ID: mdl-34581188
ABSTRACT
Background:
Angiogenesis deregulation is often linked to cancer and is thus an essential target. Materials &methods:
Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity.Results:
B1, PB11 and PB16 showed HUVEC's IC50 scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies.Conclusion:
These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Neovascularização Fisiológica
/
Inibidores da Angiogênese
/
Tiazolidinedionas
/
Inibidores de Proteínas Quinases
/
Desenvolvimento de Medicamentos
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Índia