Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1, 2, 3-triazoles as inhibitor of HER2 tyrosine kinase

ZY Cheng, WJ Li, F He, JM Zhou, XF Zhu

Index: Cheng, Zhi-Yi; Li, Wen-Jie; He, Feng; Zhou, Jun-Min; Zhu, Xiao-Feng Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 3 p. 1533 - 1538

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Citation Number: 42

Abstract

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 μM and the IC50 value of cell growth inhibition is correspondingly 30.9 μM. The lipophilicity of ...

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