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.
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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.
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.