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 

机构地区：[1]School of Pharmaceutical Sciences, Taishau Medical University, Taian 2 71016, P. R. China

出　　处：《Chemical Research in Chinese Universities》2016年第6期929-937,共9页高等学校化学研究（英文版）

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.

关 键 词：2-Aminotlfiazole ANTITUMOR activity STRUCTURE-ACTIVITY RELATIONSHIP 

分 类 号：O[理学]