Design, synthesis and antitumor evaluation of a new series of N-substituted-thiourea derivatives.
Acta Pharmacol Sin
; 27(9): 1259-71, 2006 Sep.
Article
em En
| MEDLINE
| ID: mdl-16923349
ABSTRACT
AIM:
To design and synthesize a novel class of protein tyrosine kinase inhibitors, featuring the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea framework.METHODS:
First, compounds 1 and 2 were identified using the virtual screening approach in conjunction with binding assay based on surface plasmon resonance. Subsequently, 3 regions of compounds 1 and 2 were selected for chemical modification. All compounds were characterized potent inhibitory activities toward the human lung adenocarcinoma cell line SPAC1.RESULTS:
Forty new compounds (1-2, 3a-g, 4a-w, and 5a-l) were designed, synthesized and bioassayed. Six compounds (1, 3e, 4l, 4w, 5a, and 5b) were found to show promising inhibitory activity against the SPAC1 tumor cell line. The inhibitory activity of compound 5a increases approximately 10 times more than that of the original compound 1.CONCLUSION:
This study provides a promising new template with potential antitumor activity.
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Coleções:
01-internacional
Temas:
Geral
/
Tipos_de_cancer
/
Pulmao
Base de dados:
MEDLINE
Assunto principal:
Tioureia
/
Proteínas Tirosina Quinases
/
Neoplasias Pulmonares
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Acta Pharmacol Sin
Assunto da revista:
FARMACOLOGIA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
China