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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
引用本文:陈辉,郑彩霞,杨玉峰,林婷婷,袁栋,徐峰.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[J].合成化学,2012,20(4):475-478.
作者姓名:陈辉  郑彩霞  杨玉峰  林婷婷  袁栋  徐峰
作者单位:台州职业技术学院生物与化学工程学院,浙江台州,318000
基金项目:台州市科技计划项目,2012浙江省大学生科技创新项目
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。

关 键 词:均四嗪  1  2  4-三唑  环合反应  抗癌活性

Synthesis and Anti-cancer Activities of Novel [ 1,2,4 ] Triazolo [ 4,3-b ] [ 1,2,4,5 ] tetrazine Derivatives
CHEN Hui , ZHENG Cai-xia , YANG Yu-feng , LIN Ting-ting , YUAN Dong , XU Feng.Synthesis and Anti-cancer Activities of Novel [ 1,2,4 ] Triazolo [ 4,3-b ] [ 1,2,4,5 ] tetrazine Derivatives[J].Chinese Journal of Synthetic Chemistry,2012,20(4):475-478.
Authors:CHEN Hui  ZHENG Cai-xia  YANG Yu-feng  LIN Ting-ting  YUAN Dong  XU Feng
Institution:(College of Biological and Chemical Engineering, Taizhou Vocational and Technical College,Taizhou 318000,Zhejiang,China)
Abstract:Six novel 1,2,4]triazolo4,3-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.
Keywords:1  2  4  5-tetrazine  1  2  4-triazole  cyclization  anticancer activity
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