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双长链大黄素季铵盐衍生物的合成及抗癌活性研究
引用本文:王聪慧,张风森,杜华东,胡建达,杨惠军,邵敬伟,袁耀锋,王文峰.双长链大黄素季铵盐衍生物的合成及抗癌活性研究[J].福州大学学报(自然科学版),2011,39(3):455-459.
作者姓名:王聪慧  张风森  杜华东  胡建达  杨惠军  邵敬伟  袁耀锋  王文峰
作者单位:福州大学化学化工学院;福建医科大学附属协和医院福建省血液病研究所;
基金项目:福建省科技厅重点资助项目(2010Y0033); 福州大学科技发展基金资助项目(2009-XQ-12)
摘    要:为了提高大黄素的抗癌活性和水溶性,通过羟基保护、NBS溴化、然后再和叔胺反应,得到两个双长链季铵盐大黄素衍生物.用红外光谱,核磁共振和元素分析表征了这两个产物的结构.这两个化合物对白血病K562和胃癌AGS、BGC细胞株的半数抑制浓度(IC50)均比大黄素的相应值明显降低,表明在大黄素的6位链接双长链季铵盐可以提高抗癌...

关 键 词:大黄素衍生物  抗癌活性  季铵盐  合成

Synthesis of double long-chain quaternary ammonium salt derivatives of emodin and research of anticancer activity
WANG Cong-hui,ZHANG Feng-sen,DU Hua-dong,HU Jian-d,YANG Hui-jun,SHAO Jing-wei,YUAN Yao-feng,WANG Wen-feng.Synthesis of double long-chain quaternary ammonium salt derivatives of emodin and research of anticancer activity[J].Journal of Fuzhou University(Natural Science Edition),2011,39(3):455-459.
Authors:WANG Cong-hui  ZHANG Feng-sen  DU Hua-dong  HU Jian-d  YANG Hui-jun  SHAO Jing-wei  YUAN Yao-feng  WANG Wen-feng
Institution:WANG Cong-hui1,ZHANG Feng-sen1,DU Hua-dong1,HU Jian-da2,YANG Hui-jun1,SHAO Jing-wei1,YUAN Yao-feng1,WANG Wen-feng1*(1.College of Chemistry and Chemical Engineering,Fuzhou University,Fuzhou,Fujian 350108,China,2.Union Hospital of Fujian Medical University,Fujian Institute of Hematology,Fujian 350001,China)
Abstract:In order to improve the anticancer activity and solubility of emodin,two double long-chain quaternary ammonium derivatives of emodin were synthesized through the hydroxyl protection,bromination with NBS and reaction with tertiary amines.Their structures were characterized by IR,1H-NMR and elemental analysis.The IC50 values of the two compounds on K562 leukemia cell and AGS,BGC tummy cancer cells are much lower than the corresponding values of emodin,which indicates that emodin can improve its anticancer act...
Keywords:emodin derivative  anticancer activity  quaternary ammonium salt  synthesis  
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