Feng Xiu E, Zhao Wan Yi, Ban Shu Rong, Zhao Cheng Xiao, Li Qing Shan, Lin Wen Han
School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, Shanxi, China; E-Mails:
Int J Mol Sci. 2011;12(9):6104-15. doi: 10.3390/ijms12096104. Epub 2011 Sep 19.
A series of new benzophenone and diphenylmethane halophenol derivatives were prepared. Their structures were established based on (1)H NMR, (13)C 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.
制备了一系列新型二苯甲酮和二苯甲烷卤代酚衍生物。基于氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）和高分辨质谱（HRMS）数据确定了它们的结构。对所有制备的化合物进行了体外蛋白酪氨酸激酶（PTK）抑制活性筛选。研究了连接基、官能团以及苯环上取代位置的修饰对PTK抑制活性的影响。十二种卤代酚表现出显著的PTK抑制活性。其中，化合物6c、6d、7d、9d、10d、11d和13d表现出比阳性对照染料木黄酮更强的活性。这些结果对构效关系进行了较为全面和明确的描述，并为卤代酚的进一步设计和结构优化提供了基础。
