Synthesis of 5-aryl-4-cyano-1H-1, 2, 3-triazoles and biological evaluation of their inhibitory action on tyrosine kinase / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1371-1375, 2009.
Artículo
en Chino
| WPRIM
| ID: wpr-344069
ABSTRACT
5-Aryl-4-cyano-1H-1, 2, 3-triazoles bearing a variety of substituting groups on 5-phenyl were synthesized. Their structures were established by MS, IR and 1H NMR spectra. The crystal structures of compounds 3f and 3m were determined by X-ray diffraction analysis. The active H of the triazole was on 1-N from the crystal structures. The compounds, designed as HER2 tyrosine kinase inhibitors, were screened for bioactivity of growth-inhibition of breast cancer MDA-MB-453 cells. The lowest IC50 value of inhibiting HER2 tyrosine kinase phosphorylation in breast cancer cells is 6.6 micromol x L(-1). The inhibiting-growth of breast cancer cells was enhanced from electron-drawing groups joining 5-phenyl on the triazole.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Patología
/
Farmacología
/
Fosforilación
/
Triazoles
/
Proteínas Tirosina Quinasas
/
Neoplasias de la Mama
/
Química
/
Cristalografía por Rayos X
/
Receptor ErbB-2
/
Cristalización
Límite:
Femenino
/
Humanos
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2009
Tipo del documento:
Artículo
Similares
MEDLINE
...
LILACS
LIS