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.
Article
in Chinese
| 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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Phosphorylation
/
Triazoles
/
Protein-Tyrosine Kinases
/
Breast Neoplasms
/
Chemistry
/
Crystallography, X-Ray
/
Receptor, ErbB-2
/
Crystallization
Limits:
Female
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Type:
Article
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