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缩胺硫脲化合物的合成及其抗癌活性的研究
引用本文:胡惟孝,孙楠,杨忠愚.缩胺硫脲化合物的合成及其抗癌活性的研究[J].高等学校化学学报,2001,22(12):2014-2017.
作者姓名:胡惟孝  孙楠  杨忠愚
作者单位:浙江工业大学制药工程研究所, 杭州 310014
基金项目:浙江省自然科学基金 (批准号 :2 0 0 0 16 )资助
摘    要:以肼基二硫代甲酸甲酯(Ⅱ)与相应的酮或醛反应,生成3-二取代甲撑基二硫代甲酸甲酯(Ⅲ).化合物与N-单取代哌嗪反应,制得不同取代基的标题化合物缩胺硫脲(Ⅰ),产率27~85.产物的结构用IR,NMR和元素分析证实,用磺酰罗丹明β蛋白染色法(SRB法)和四氮唑盐还原法(MTT法)检验了它们对鼠白血病(P-388)和人肺癌(A-549)细胞株的抑制活性.

关 键 词:缩胺硫脲  抗癌活性  有机合成  肼基二硫代甲酸甲酯  
文章编号:0251-0790(2001)12-2014-04
收稿时间:2000-07-08
修稿时间:2000年7月8日

Studies on Synthesis and Anticancer Activity of Thiosemicarbazones
HU Wei Xiao ,SUN Nan,YANG Zhong Yu.Studies on Synthesis and Anticancer Activity of Thiosemicarbazones[J].Chemical Research In Chinese Universities,2001,22(12):2014-2017.
Authors:HU Wei Xiao  SUN Nan  YANG Zhong Yu
Institution:Institute of Pharmaceutical Engineering, Zhejiang University of Technology, Hangzhou 310014, China
Abstract:Sixteen of thiosemicarbazone(Ⅰ) was synthesized. Hydrazine reacts with carbondisulfide and dimethyl sulfate in the presence of potassium hydroxide to form compound Ⅱ with yield 60. compound Ⅱ reacts with ketone or aldehyde to form compound Ⅲ. Compound Ⅲ reacts with Nsubstituted piperazine to form Ⅰ with yield 27-85. The structures of the compounds were comfirmed by IR, NMR, elemental analysis, and the results shows that the thiosemicarbazone with proper substituents has somewhat activity. These compounds are valuable ones for being studied further.
Keywords:Thiosemicarbazone  Anticancer activity  Organic synthesis  Methyl hydrazinecarbodithioate
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