| 内盐式磷酯替加氟缀合物的合成与抗癌活性 |
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| 引用本文： | 张尊英,刘少琼,臧中林,李言杰,许新华. 内盐式磷酯替加氟缀合物的合成与抗癌活性[J]. 合成化学, 2007, 15(2): 192-194 |
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| 作者姓名： | 张尊英 刘少琼 臧中林 李言杰 许新华 |
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| 作者单位： | 湖南大学,化学化工学院,湖南,长沙,410082;中南大学,湘雅二医院,湖南,长沙,410083 |
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| 基金项目： | 国家自然科学基金资助项目(20372020) |
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| 摘 要： | 2-(N,N二-乙基氨基)-1,3,2二-氧磷杂环戊烷与羟烷基替加氟及硫反应得中间体2,三乙胺对2开环得内盐式磷酯替加氟缀合物3。2和3的结构经1H NMR,31P NMR和元素分析表征。初步抗癌活性测试结果表明,3对膀胱癌细胞T-24与胃癌细胞BGC-823有一定的抑制作用。
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| 关 键 词： | 替加氟 内盐式磷酸酯 合成 抗癌活性 |
| 文章编号： | 1005-1511（2007）02-0192-03 |
| 收稿时间： | 2006-10-16 |
| 修稿时间： | 2006-10-16 |
Synthesis and Antitumor Activity of Conjugate of Phosphate Zwitterions and Tegafur |
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| ZHANG Zun-ying,LIU Shao-qiong,ZANG Zhong-lin,LI Yan-jie,XU Xin-hua. Synthesis and Antitumor Activity of Conjugate of Phosphate Zwitterions and Tegafur[J]. Chinese Journal of Synthetic Chemistry, 2007, 15(2): 192-194 |
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| Authors: | ZHANG Zun-ying LIU Shao-qiong ZANG Zhong-lin LI Yan-jie XU Xin-hua |
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| Affiliation: | 1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China; 2. Xiangya Second Hospital, Center South University, Changsha 410083, China |
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| Abstract: | Intermediate 2 was synthesized by one-pot reaction of 2-(N,N-diethylamino)-1,3,2-dioxaphospholane and N1-(2-furanidyl)-N3-(hydroxyalkyl)-5-fluyorouracil and sulfur.2 reacted with triethylamine to obtain conjugate of phosphate zwitterions and tegafur(3).The structures of 2 and 3 were confirmed by 1H NMR,31P NMR and elemental analysis.3 exhibited antitumor activity against human urinaryl bladder cancer cell T-24 and stomach cancer cell BGC-823. |
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| Keywords: | tegafur phosphate zwitterions synthesis antitumor activity |
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