新型[1,2,4]三唑[4,3-b]均四嗪类化合物的合成及其抗癌活性  

Synthesis and Anti-cancer Activities of Novel[1,2,4]Triazolo[4,3-b][1,2,4,5]tetrazine Derivatives

作　　者：陈辉[1] 郑彩霞[1] 杨玉峰[1] 林婷婷[1] 袁栋[1] 徐峰[1] 

机构地区：[1]台州职业技术学院生物与化学工程学院,浙江台州318000

出　　处：《合成化学》2012年第4期475-478,共4页Chinese Journal of Synthetic Chemistry

基　　金：台州市科技计划项目(20111ky01);2012浙江省大学生科技创新项目(2012DKC02)

摘　　要：以6-(3,5-二甲基吡唑-1-基)-3-肼基均四嗪和芳醛为原料,经Schiff碱缩合和环合反应合成了6个新型的6-芳基-3-(3,5-二甲基吡唑-1-基)[1,2,4]三唑[4,3-b]均四嗪类化合物(4a～4f),其结构经1HNMR,MS,IR和元素分析表征。以顺铂为对照,采用MTT法测试了体外4a～4f对人白血病细胞株,人肺癌,人乳腺癌和人子宫颈癌细胞株的抗癌活性。结果表明,4a～4f对四种癌细胞均具有较强的抑制活性。Six novel [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine compounds（4a^4f） were synthesized by Schiff base condensation and cyclization from 3- （3,5-dimethyl-1H-pyrazol-1-yl）-6-hydrazinyl-1,2,4,5-tetrazine and aromatic aldehyde.The structures were characterized by 1H NMR,MS,IR and elemental analysis.The anti-cancer activities of 4a-4f against HL-60,A -549,MCF-7 and Hela cell lines（cisplatin as a control） in vitro by MTT method were investigated.The results showed that 4a-4f exhibited strong anticancer activities in vitro against four cancer cell.

关 键 词：均四嗪 1 2 4-三唑 环合反应 抗癌活性 

分 类 号：O626.44[理学—有机化学] R914.5[理学—化学]