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

International Journal of Molecular Sciences

Xiu E. Feng¹  Wan Yi Zhao¹  Shu Rong Ban¹  Cheng Xiao Zhao¹  Qing Shan Li¹ 

[1] School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, Shanxi, China; E-Mails:

关键词: protein tyrosine kinase;    halophenol;    structure-activity relationship;    benzophenone;    diphenylmethane;   

DOI  :  10.3390/ijms12096104

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.