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Int. J. Mol. Sci. 2011, 12(9), 6104-6115; doi:10.3390/ijms12096104
Article

Structure–Activity Relationship of Halophenols as a New Class of Protein Tyrosine Kinase Inhibitors

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Received: 25 May 2011 / Revised: 14 September 2011 / Accepted: 15 September 2011 / Published: 19 September 2011
(This article belongs to the Section Bioactives and Nutraceuticals)
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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 protein tyrosine kinase; halophenol; structure–activity relationship; benzophenone; diphenylmethane
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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