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
收稿日期: 2017-09-19
修回日期: 2017-10-25
网络出版日期: 2017-11-17
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
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).
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.
栗娜 , 辛景超 , 马启胜 , 李二冬 , 孟娅琪 , 包崇男 , 杨鹏 , 宋攀攀 , 崔飞 , 陈鹏举 , 顾一飞 , 赵培荣 , 可钰 , 刘宏民 , 张秋荣 . 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[J]. 有机化学, 2018 , 38(3) : 665 -671 . DOI: 10.6023/cjoc201709030
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
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