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Chinese Journal of Organic Chemistry >

2018 , Vol. 38 >Issue 3: 665 - 671

DOI: https://doi.org/10.6023/cjoc201709030

Articles

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

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

Received date: 2017-09-19

  Revised date: 2017-10-25

  Online published: 2017-11-17

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).

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

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