Design, Synthesis, Inhibiting HDACs Ability and Antitumor Activity of Pyrimidin-4（3H）-one Hydroxamate Derivatives

作     者：LU Haibin JIN Xiangqun JIN Yang HUANG Bangrui WANG Cheng WANG Chunhe MA Fangyuan CHEN Yuting LI Jiarui CONG Yu WANG Wenlong SONG Yuming MU Xupeng 

作者机构：College of Pharmacy Jilin University Changchun 130021 P. R. China China-Japan Union Hospital of Jilin University Changchun 130033 P. R. China 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2016年第32卷第4期

页      面：576-580页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 0703[理学-化学] 070301[理学-无机化学] 10[医学] 

基　　金：Supported by the National Natural Science Foundation of China(No.31540082) 

主　　题：Histone deacetylase Antitumor acitivty Pyrimidin-4(3H)-one hydroxamate derivative 

摘      要：A series of novel pyrimidin-4（3H）-one hydroxamate derivatives was designed, synthesized and studied for their activities against histone deacetylases（HDACs）. The results indicate that all the compounds show HDACs inhibitiory activity. The antiproliferative activities of the compounds against HeLa and A549 cells were also investigated. The pharmacological results show compound 9g has potent activity in the enzymatic inhibition assay and cell-based assay.