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| O-(1-芳硒基-3-铵基)异丙基-O-2-(N3-替加氟)乙基硫代磷酯的合成与活性 | |
| 引用本文： | 刘少琼,陆振荣,臧中林,李言杰,许新华. O-(1-芳硒基-3-铵基)异丙基-O-2-(N3-替加氟)乙基硫代磷酯的合成与活性[J]. 中国药物化学杂志, 2007, 17(4): 217-220 |
| 作者姓名： | 刘少琼 陆振荣 臧中林 李言杰 许新华 |
| 作者单位： | 1. 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,410011 2. 湖南大学,化学化工学院,湖南,长沙,410082;湖南永利化工股份有限公司,湖南,株洲,412004 3. 湖南大学,化学化工学院,湖南,长沙,410082 |
| 摘 要： | 目的合成O-(1-芳硒基-3-铵基)异丙基-O-2-(N3-替加氟)乙基硫代磷酯,并测定其活性。方法六乙基亚磷酰三胺依次与羟乙基替加氟、1-芳硒基甘油及硫反应,得到环甘油硫代磷替加氟缀合物,分别通过三乙胺及三甲胺对其进行亲核开环,得到目标产物。结果与结论得到12个新化合物,其结构经过1H-NMR、31P-NMR及元素分析确证。目标化合物对膀胱癌细胞PGA1、胃癌细胞BGC-823有一定的抑制作用。 |
| 关 键 词： | 替加氟 有机硒 内盐式磷酸酯 抗癌活性 |
| 文章编号： | 1005-0108（2007）04-0217-04 |
| 收稿时间： | 2007-01-26 |
| 修稿时间： | 2007-01-26 |
Synthesis and antitunor activity of O-(1-arylseleno-3- ammonium) isopropyl-O-2-(N3-tegafur) ethyl thiophosphate |
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| LIU Shao-qiong,LU Zhen-rong,ZANG Zhong-lin,LI Yan-jie,XU Xin-hua. Synthesis and antitunor activity of O-(1-arylseleno-3- ammonium) isopropyl-O-2-(N3-tegafur) ethyl thiophosphate[J]. Chinese Journal of Medicinal Chemistry, 2007, 17(4): 217-220 | |
| Authors: | LIU Shao-qiong LU Zhen-rong ZANG Zhong-lin LI Yan-jie XU Xin-hua |
| Affiliation: | 1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China ; 2. Xiangya Second Hospital, Center South University, Changsha 410011, China ; 3. Hunan Yongli Chemical Industry Co., Ltd., Zhuzhou 412004, China |
| Abstract: | Aim To synthesize O-(1-arylseleno-3-ammonium) isopropyl-O-2-(N3-tegafur) ethyl thiophosphate and test their antitumor activities.Methods Hexaethylphosphorous triamide was treated with N1-(2-furanidyl)-N3-(hydroxyethyl)-5-fluyorouracil and 1-seleniumaryl glycerol as well as sulfur in one-pot to give intermediates 2a-2d.2a-2d reacted respectively with triethylamine and trimethylamine to give title compounds 3a-3h.Results and conclusion Twelve new compounds were synthesized.Their structure were confirmed by 1H-NMR,31P-NMR,and elemental analysis.3a-3h show high antitumor activities against human uriaryl bladder cancer cell PGA1 and BGC-823. |
| Keywords: | tigafur organic selenium phosphate zwitterions antitumor activity |
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