摘要/Abstract

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


PDF全文下载地址:

点我下载PDF