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

doi:10.1007/s40242-016-6304-2

高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (6): 929-937.doi: 10.1007/s40242-016-6304-2

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

LI Hongshuang, WANG Xinran, DUAN Guiyun, XIA Chengcai, XIAO Yuliang, LI Furong, GE Yanqing, YOU Guirong, HAN Junfen, FU Xiaopan, TAN Shanhui, WANG Rongwei

School of Pharmaceutical Sciences, Taishan Medical University, Taian 271016, P. R. China

收稿日期:2016-07-14 修回日期:2016-10-19 出版日期:2016-12-01 发布日期:2016-11-28
通讯作者: DUAN Guiyun, E-mail:duanguiyun@126.com E-mail:duanguiyun@126.com
基金资助:
Supported by the Science and Technology Development Project of Shandong Province, China(No.2012GSF11812), the Natural Science Foundation of Shandong Province, China(No.ZR2015BL006) and the Project of Shandong Province Higher Educational Science and Technology Program, China(No.J15LM08).

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

LI Hongshuang, WANG Xinran, DUAN Guiyun, XIA Chengcai, XIAO Yuliang, LI Furong, GE Yanqing, YOU Guirong, HAN Junfen, FU Xiaopan, TAN Shanhui, WANG Rongwei

School of Pharmaceutical Sciences, Taishan Medical University, Taian 271016, P. R. China

Received:2016-07-14 Revised:2016-10-19 Online:2016-12-01 Published:2016-11-28
Contact: DUAN Guiyun, E-mail:duanguiyun@126.com E-mail:duanguiyun@126.com
Supported by:
Supported by the Science and Technology Development Project of Shandong Province, China(No.2012GSF11812), the Natural Science Foundation of Shandong Province, China(No.ZR2015BL006) and the Project of Shandong Province Higher Educational Science and Technology Program, China(No.J15LM08).

摘要/Abstract

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 μmol/L against the two tested cell lines, respectively. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated.

关键词: 2-Aminothiazole, Antitumor activity, Structure-activity relationship

Abstract:

Key words: 2-Aminothiazole, Antitumor activity, Structure-activity relationship

LI Hongshuang, WANG Xinran, DUAN Guiyun, XIA Chengcai, XIAO Yuliang, LI Furong, GE Yanqing, YOU Guirong, HAN Junfen, FU Xiaopan, TAN Shanhui, WANG Rongwei. Synthesis, Antitumor Activity and Preliminary Structure-activity Relationship of 2-Aminothiazole Derivatives[J]. 高等学校化学研究, 2016, 32(6): 929-937.

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

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

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