有机化学 ›› 2018, Vol. 38 ›› Issue (3): 665-671.DOI: 10.6023/cjoc201709030 上一篇    下一篇

研究论文

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   

  1. 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 Naa,b, Xin Jingchaoa,b, Ma Qishenga,b, Li Erdonga,b, Meng Yaqia,b, Bao Chongnana,b, Yang Penga,b, Song Panpana,b, Cui Feia,b, Cheng Pengjua, Gu Yifeia, Zhao Peirongb, Ke Yua,b, Liu Hongmina,b, Zhang Qiuronga,b   

  1. 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).

为了寻找高效的抗肿瘤药物,设计并合成了一系列新型的1,2,3-三氮唑[4,5-d]嘧啶类衍生物,对这些化合物在人类五种癌细胞MGC-803(人胃癌细胞)、MCF-7(人乳腺癌细胞)、EC-109(人食管癌细胞)、PC-3(人前列腺癌细胞)、Hela(人宫颈癌细胞)进行抗肿瘤活性评价,结果显示大部分化合物具有较好的抗肿瘤活性,其中5-(((1H-苯并[d]咪唑-2-基)甲基)硫基)-3-苄基-N-(4-氯苯基)-3H-[1,2,3]-三氮唑[4,5-d]嘧啶-7-胺(11b)和2,2'-((5-(((1H-苯并[d]咪唑-2-基)甲基)硫基)-3-苄基-3H-[1,2,3]-三氮唑[4,5-d]嘧啶-7-基)氮烷二基)双(乙烷-1-醇)(11m)对MGC-803和Hela癌细胞的抗肿瘤活性优于对照品氟尿嘧啶.

关键词: 三氮唑, 嘧啶, 抗肿瘤活性, 衍生物, 评价

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