Synthesis, Antitumor Activity and Preliminary Structure-activity Relationship of 2-Aminothiazole Derivatives

作     者：LI Hongshuang WANG Xinran DUAN Guiyun XIA Chengcai XIAO Yuliang LI Furong GE Yanqing YOU Guirong HAN Junfen FU Xiaopan 

作者机构：School of Pharmaceutical Sciences Taishau Medical University Taian 2 71016 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6期

页      面：929-937页

核心收录：

学科分类：07[理学] 

基　　金：Supported by the Science and Technology Development Project of Shandong Province, China 山东省自然科学基金 the Project of Shandong Province Higher Educational Science and Technology Program, China 

主　　题：2-Aminotlfiazole Antitumor activity Structure-activity relationship 

摘      要：In this paper, we described the synthesis of 2-aminoflfiazole sublibrary containing methyl, bromo, phenylor butylidene at 4- or/and 5-position of its core. All target compounds were evaluated tbr their antitumor activitiesagainst human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compotmds screened,4,5,6,7-tetrahydrobenzo[d]thiazole（26b） exhibited the most potent antittunor activities with IC50 values of 4.89 and4.03 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship（SAR） studies ofthese compound were subsequently investigated.