期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 15, 期 3, 页码 1533-1538出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.09.041
关键词
1,2,3-triazole; tyrosine kinase inhibitor; breast cancer
4-Aryl-5-cyano-2H-1,2,3-triazoles bearing a variety of substituting groups on 4-phenyl were synthesized. The chemicals, designed as HER2 tyrosine kinase inhibitors, were screened for bioactivity of inhibiting growth of breast cancer MDA-MB-453 cells. The lowest IC50 value of inhibiting HER2 tyrosine kinase phosphorylation in breast cancer cells is 6.6 mu M and the IC50 value of cell growth inhibition is correspondingly 30.9 mu M. The lipophilicity of substituting groups on triazoles is the main factor to influence their bioactivities. (c) 2006 Elsevier Ltd. All rights reserved.
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