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

• Published in: Chemical research in Chinese universities Vol. 32; no. 6; pp. 929 - 937
• Main Authors: Li, Hongshuang, Wang, Xinran, Duan, Guiyun, Xia, Chengcai, Xiao, Yuliang, Li, Furong, Ge, Yanqing, You, Guirong, Han, Junfen, Fu, Xiaopan, Tan, Shanhui, Wang, Rongwei
• Format: Journal Article
• Language: English
• Published: Changchun Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01.12.2016; Springer Nature B.V
• Subjects: 2-Aminotlfiazole; activity; Analytical Chemistry; Anticancer properties; Antitumor; Bioactive; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Inorganic Chemistry; Organic Chemistry; Physical Chemistry; relationship; Structure-activity; Synthesis; 2-Aminothiazole; Antitumor activity; Structure-activity relationship
• ISSN: 1005-9040; 2210-3171
• DOI: 10.1007/s40242-016-6304-2

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.