Citation: 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]. Chinese Journal of Organic Chemistry, ;2018, 38(3): 665-671. doi: 10.6023/cjoc201709030 shu

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,,

1.
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
2.
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou 450001

Corresponding author: Ke Yu, ky@zzu.edu.cn Liu Hongmin, liuhm@zzu.edu.cn Zhang Qiurong, zqr406@sina.com
Received Date: 19 September 2017
Revised Date: 25 October 2017
Available Online: 17 March 2017
Fund Project: the Research Project of Science and Technology Bureau of Zhengzhou City 141PQYJS554the National Natural Science Foundation of China 81430085Project 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)

Figures(2)

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.
- triazolo,
- pyrimidine,
- antitumor activity,
- derivatives,
- evaluate
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