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

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

1
School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, Shanxi, China
2
School of Public Health, Shanxi Medical University, Taiyuan 030001, Shanxi, China
3
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China
*
Author to whom correspondence should be addressed.
Received: 25 May 2011 / Revised: 14 September 2011 / Accepted: 15 September 2011 / Published: 19 September 2011
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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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. View Full-Text
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 (CC BY 3.0).

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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.

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