Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-d]pyrimidine Derivatives

doi:10.6023/cjoc201709030

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (3): 665-671.DOI: 10.6023/cjoc201709030 Previous Articles Next Articles

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1,2,3-三氮唑[4,5-d]嘧啶衍生物的合成及抗肿瘤活性评价

栗娜^a,b, 辛景超^a,b, 马启胜^a,b, 李二冬^a,b, 孟娅琪^a,b, 包崇男^a,b, 杨鹏^a,b, 宋攀攀^a,b, 崔飞^a,b, 陈鹏举^a, 顾一飞^a, 赵培荣^b, 可钰^a,b, 刘宏民^a,b, 张秋荣^a,b

a 郑州大学药学院郑州 450001;
b 新药创制与药物安全性评价河南省协同创新中心郑州 450001

收稿日期:2017-09-19 修回日期:2017-10-25 发布日期:2017-11-17
通讯作者: 可钰,E-mail:ky@zzu.edu.cn;刘宏民,E-mail:liuhm@zzu.edu.cn;张秋荣,E-mail:zqr406@sina.com E-mail:ky@zzu.edu.cn;liuhm@zzu.edu.cn;zqr406@sina.com
基金资助:
国家自然科学基金（No.81430085）和郑州市科技局科研（No.141PQYJS554）资助项目.

Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-d]pyrimidine Derivatives

Li Na^a,b, Xin Jingchao^a,b, Ma Qisheng^a,b, Li Erdong^a,b, Meng Yaqi^a,b, Bao Chongnan^a,b, Yang Peng^a,b, Song Panpan^a,b, Cui Fei^a,b, Cheng Pengju^a, Gu Yifei^a, Zhao Peirong^b, Ke Yu^a,b, Liu Hongmin^a,b, Zhang Qiurong^a,b

a School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
b Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001

Received:2017-09-19 Revised:2017-10-25 Published:2017-11-17
Contact: 10.6023/cjoc201709030 E-mail:ky@zzu.edu.cn;liuhm@zzu.edu.cn;zqr406@sina.com
Supported by:
Project supported by the National Natural Science Foundation of China (No. 81430085)and the Research Project of Science and Technology Bureau of Zhengzhou City (No.141PQYJS554).

1. Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-d]pyrimidine Derivatives.PDF(2054KB)

Abstract

In order to find more efficient and economical antitumor drugs, a series of novel 1,2,3-triazolo[4,5-d]pyrimidine derivatives were synthesized and evaluated for their antitumor activities against five human cancer cell lines (MGC-803, MCF-7, EC-109, PC-3 and Hela) in vitro. The results showed that most compounds had good antitumor activities, especially 5-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-3-bezyl-N-(4-chlorophenyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine (11b) and 2,2'-((5-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-3-benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)azanediyl)bis(ethan-1-ol) (11m) exhibited better antitumor activities than 5-fluorouracil against MGC-803 and Hela.

Key words: triazolo, pyrimidine, antitumor activity, derivatives, evaluate

Cite this article

Li Na, Xin Jingchao, Ma Qisheng, Li Erdong, Meng Yaqi, Bao Chongnan, Yang Peng, Song Panpan, Cui Fei, Cheng Pengju, Gu Yifei, Zhao Peirong, Ke Yu, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-d]pyrimidine Derivatives[J]. Chin. J. Org. Chem., 2018, 38(3): 665-671.

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1,2,3-三氮唑[4,5-d]嘧啶衍生物的合成及抗肿瘤活性评价

Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-d]pyrimidine Derivatives

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