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Structure–Activity Relationship of Halophenols as a New Class of Protein Tyrosine Kinase Inhibitors
School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, Shanxi, China
School of Public Health, Shanxi Medical University, Taiyuan 030001, Shanxi, China
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China
* Author to whom correspondence should be addressed.
Received: 25 May 2011; in revised form: 14 September 2011 / Accepted: 15 September 2011 / Published: 19 September 2011
Abstract: A series of new benzophenone and diphenylmethane halophenol derivatives were prepared. Their structures were established based on 1H NMR, 13C NMR and HRMS data. All prepared compounds were screened for their in vitro protein tyrosine kinase (PTK) inhibitory activities. The effects of modification of the linker, functional groups and substituted positions at the phenyl ring on PTK inhibitory activity were investigated. Twelve halophenols showed significant PTK inhibitory activity. Among them, compounds 6c, 6d, 7d, 9d, 10d, 11d and 13d exhibited stronger activities than that of genistein, the positive reference compound. The results gave a relatively full and definite description of the structure–activity relationship and provided a foundation for further design and structure optimization of the halophenols.
Keywords: protein tyrosine kinase; halophenol; structure–activity relationship; benzophenone; diphenylmethane
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MDPI and ACS Style
Feng, X.E.; Zhao, W.Y.; Ban, S.R.; Zhao, C.X.; Li, Q.S.; Lin, W.H. Structure–Activity Relationship of Halophenols as a New Class of Protein Tyrosine Kinase Inhibitors. Int. J. Mol. Sci. 2011, 12, 6104-6115.
Feng XE, Zhao WY, Ban SR, Zhao CX, Li QS, Lin WH. Structure–Activity Relationship of Halophenols as a New Class of Protein Tyrosine Kinase Inhibitors. International Journal of Molecular Sciences. 2011; 12(9):6104-6115.
Feng, Xiu E; Zhao, Wan Yi; Ban, Shu Rong; Zhao, Cheng Xiao; Li, Qing Shan; Lin, Wen Han. 2011. "Structure–Activity Relationship of Halophenols as a New Class of Protein Tyrosine Kinase Inhibitors." Int. J. Mol. Sci. 12, no. 9: 6104-6115.