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

被引：7

作者：

Li Hongshuang ^{[1
]}

Wang Xinran ^{[1
]}

Duan Guiyun ^{[1
]}

Xia Chengcai ^{[1
]}

Xiao Yuliang ^{[1
]}

Li Furong ^{[1
]}

Ge Yanqing ^{[1
]}

You Guirong ^{[1
]}

Han Junfen ^{[1
]}

Fu Xiaopan ^{[1
]}

Tan Shanhui ^{[1
]}

Wang Rongwei ^{[1
]}

机构：

[1] Taishan Med Univ, Sch Pharmaceut Sci, Tai An 271016, Shandong, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2016年 / 32卷 / 06期

关键词：

2-Aminothiazole; Antitumor activity; Structure-activity relationship; CYCLIN-DEPENDENT KINASE; BIOLOGICAL EVALUATION; THIAZOLE DERIVATIVES; POTENTIAL ANTITUMOR; INHIBITORS; DESIGN; AGENTS; DISCOVERY; ANALOGS; BMS-354825;

D O I：

10.1007/s40242-016-6304-2

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this paper, we described the synthesis of 2-aminothiazole sublibrary containing methyl, bromo, phenyl or butylidene at 4-or/and 5-position of its core. All target compounds were evaluated for their antitumor activities against human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compounds screened, 4,5,6,7-tetrahydrobenzo[d] thiazole(26b) exhibited the most potent antitumor activities with IC50 values of 4.89 and 4.03 mu mol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated.

引用

页码：929 / 937

页数：9

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