[Synthesis of 5-aryl-4-cyano-1H-1, 2, 3-triazoles and biological evaluation of their inhibitory action on tyrosine kinase].
Yao Xue Xue Bao
; 44(12): 1371-5, 2009 Dec.
Article
em Zh
| MEDLINE
| ID: mdl-21351471
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.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Proteínas Tirosina Quinases
/
Neoplasias da Mama
/
Receptor ErbB-2
Limite:
Female
/
Humans
Idioma:
Zh
Ano de publicação:
2009
Tipo de documento:
Article