| (S/R)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸的合成及抗肿瘤活性 |
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| 引用本文： | 江吉旺,晁国库,王璐,王紫怡,周书光,徐静,熊静. (S/R)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸的合成及抗肿瘤活性[J]. 化学世界, 2011, 52(8) |
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| 作者姓名： | 江吉旺 晁国库 王璐 王紫怡 周书光 徐静 熊静 |
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| 作者单位： | 温州大学化学与材料工程学院,浙江温州,325035 |
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| 基金项目： | 浙江省大学生科技创新活动计划(新苗人才计划)项目(2010R424046;2010R424013); 浙江省科技计划项目(2009C33059); 温州市科技计划项目(Y20100003) |
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| 摘 要： | 以1-乙基-3-(3-二甲胺丙基)碳二亚胺盐酸盐(EDCI)/1-羟基苯并三氮唑(HOBt)为缩合剂,5-氟尿嘧啶-1-基乙酸为中间体,分别与L-酪氨酸甲酯和D-酪氨酸乙酯通过液相偶联合成了(S)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸甲酯和(R)-2-(2-(5-氟-2,4-二氧-3,4-二氢嘧啶-1(2H)-基)乙酰氨基)-3-(4-羟苯基)丙酸乙酯,水解后得到相应的酸对映体。所合成的化合物结构经1H NMR1、3C NMRI、R、MS及比旋光度等测试得以确证。四种化合物的体外抗肿瘤活性测试结果,说明该化合物的抗肿瘤具有一定的选择性,且R构型对抗肿瘤也起到了一定的作用。
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| 关 键 词： | 5-氟尿嘧啶 酪氨酸 液相偶联 结构表征 抗肿瘤 |
Synthesis and Antitumor Activities of(S/R)-2-(2-(5-Fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl) acetamido)-3-(4-hydroxyphenyl)propanoic Acid |
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| JIANG Ji-wang,CHAO Guo-ku,WANG Lu,WANG Zi-yi,ZHOU Shu-guang,XU Jing,XIONG Jing. Synthesis and Antitumor Activities of(S/R)-2-(2-(5-Fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl) acetamido)-3-(4-hydroxyphenyl)propanoic Acid[J]. Chemical World, 2011, 52(8) |
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| Authors: | JIANG Ji-wang CHAO Guo-ku WANG Lu WANG Zi-yi ZHOU Shu-guang XU Jing XIONG Jing |
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| Affiliation: | JIANG Ji-wang,CHAO Guo-ku,WANG Lu,WANG Zi-yi,ZHOU Shu-guang,XU Jing,XIONG Jing(College of Chemistry & Materials Engineering,Wenzhou University,Zhejiang Wenzhou 325035,China) |
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| Abstract: | (S)-Methyl 2-(2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamido)-3-(4-hydroxy phenyl)propanoate and(R)-ethyl 2-(2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamido)-3-(4-hydroxyphenyl)propanoate were synthesized from L-tyrosine methyl ester and D-tyrosine ethyl ester,respectively,with EDCI/HOBt as a coupling reagent and 5-flurouracil-1-yl acetic acid as an intermediate.The corresponding acid enantiomers were obtained after hydrolysis.The structures of the compounds were characterized b... |
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| Keywords: | 5-fluorouracil tyrosine liquid coupling characterization antitumor |
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