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缩胺硫脲类化合物的合成及其抗癌活性研究
引用本文:胡惟孝,孙楠,杨忠愚. 缩胺硫脲类化合物的合成及其抗癌活性研究[J]. 中国药物化学杂志, 2001, 11(3): 129-133
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,
摘    要:合成了16个新型缩胺硫脲类化合物。先由硫酸二甲酯、水合肼与二硫化碳反应,生成肼基二硫代甲酸甲酯(Ⅱ),产率为60%。取代芳香酮、醛与Ⅱ反应,制备中间体Ⅲ,收率:51%-91%。Ⅲ与N-取代哌嗪反应制备目标代合物Ⅰ,收率:27.3%-85.7%。其结构经IR、^1H-NMR和元素分析等确证。体外抗癌活性测定表明,在适当的基代基匹配下,此类化合物有一定的抗癌活性。

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:1005-0108(2001)03-0129-05

A Study on Synthesis andAnticancer Activity of Thiosemicarbazones
HU Wei-xiao,SUN Nan,YANG Zhong-yu. A Study on Synthesis andAnticancer Activity of Thiosemicarbazones[J]. Chinese Journal of Medicinal Chemistry, 2001, 11(3): 129-133
Authors:HU Wei-xiao  SUN Nan  YANG Zhong-yu
Abstract:Sixteen of thiosemicarbazones Ⅰ were synthesized.Hydrazine reacted with carbon disulfide and dimethyl sulfate in the presence of potassium hydroxide to form compound(Ⅱ) with the yield of 60%.Ⅱ reacted with ketone or aldehyde to form Ⅲ with the yield of 51%~91%.Ⅲ reacted with N-substitued piperazine to form Ⅰ with the yield of 27%~85%.Their structures of the compounds were comfirmed by IR,1H-NMR,elemental analysis,and the results showed that the thiosemicarbazone with proper substituents had somewhat activity.It is a valuable compound to be researched further.
Keywords:thiosemicarbazone  anticancer activity  organic synthesis  methyl hydrazinecarbodithioate
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