| 8-羟基喹啉-7-醛缩氨基硫脲衍生物的微波合成及抗肿瘤活性研究 |
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| 引用本文： | 时蕾,刘艳春,王振平,张贵生.8-羟基喹啉-7-醛缩氨基硫脲衍生物的微波合成及抗肿瘤活性研究[J].化学研究与应用,2012(7):1141-1146. |
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| 作者姓名： | 时蕾 刘艳春 王振平 张贵生 |
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| 作者单位： | 绿色化学介质与反应教育部重点实验室,河南师范大学化学与环境科学学院 |
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| 基金项目： | 国家自然科学基金项目(21172056)资助;长江学者和创新团队发展计划项目(IRT1061)资助;河南省科学厅科技攻关项目(092102310115)资助 |
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| 摘 要： | 以8-羟基喹啉-7-醛和一系列芳基及烷基取代氨基硫脲为原料,合成了15种8-羟基喹啉缩氨基硫脲类化合物。缩合反应在绿色溶剂水中进行,微波辐射下15-30 min内反应完全,操作简单,收率高。化合物结构经1H NMR、IR和高分辨质谱确证。部分化合物经抗肿瘤活性初步测试结果表明,多数化合物对细胞周期分裂蛋白25B(CDC25B)抑制率达到90%以上,具有潜在的抗肿瘤活性。
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| 关 键 词： | 8-羟基喹啉-7-醛缩氨基硫脲 微波辐射 绿色合成 抗肿瘤活性 |
Microwave-enhanced synthesis and antitumor activity of 8-hydroxyquinoline-7-aldehyde thiosemicarbazones |
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| SHI Lei,LIU Yan-chun,WANG Zhen-ping,ZHANG Gui-sheng.Microwave-enhanced synthesis and antitumor activity of 8-hydroxyquinoline-7-aldehyde thiosemicarbazones[J].Chemical Research and Application,2012(7):1141-1146. |
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| Authors: | SHI Lei LIU Yan-chun WANG Zhen-ping ZHANG Gui-sheng |
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| Institution: | *(Key Laboratory of Green Chemical Media and Reactions,Ministry of Education,College of Chemistry and Environmental Science,Henan Normal University,Xinxiang 453007,China) |
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| Abstract: | Fifteen 8-hydroxyquinoline-7aldehyde thiosemicarbazones were synthesized via the condensation of 8-hydroxyquinolin-7-aldehyde and aryl or alkyl thiosemicarbazides.The reactions were completed in 15-30min under the microwave radiation in neat water and the products were obtained in excellent yields after simple operation.The structures were identified by 1HNMR,IR and HRMS(ESI).The preliminary results indicated that most compounds possess high inhibiting activity against CDC 25B,and showed potential antitumor activity. |
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| Keywords: | 8-hydroxyquinoline-7-aldehyde microwave radiation green synthesis antitumor activity |
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