| 5-氟尿嘧啶的三元环类化合物的缀合物的合成及其抗肿瘤活性 |
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| 引用本文： | 王 乐,张运晓,陶京朝.5-氟尿嘧啶的三元环类化合物的缀合物的合成及其抗肿瘤活性[J].中国化学,2009,27(7):1374-1378. |
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| 作者姓名： | 王 乐 张运晓 陶京朝 |
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| 作者单位： | 郑州大学化学系新药研究开发中心，郑州 450052 |
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| 摘 要： | 基于具有三元环状结构的化合物的广泛生理活性和氟尿嘧啶的抗癌作用机制，本文设计、合成并表征了一系列新型5-氟尿嘧啶（5-FU）的三元碳环缀合物及三元氧杂环缀合物。并对5-FU 的N-1和N-3位的选择性烷基化方法进行了系统研究，发现苄氧甲酰氧甲基保护基具有稳定性高、有效保护性好、制备方便、易于脱除等特点，适宜于在本类反应中应用。测试了所合成的新型5-FU三元环缀合物的体外抗肿瘤活性，化合物7、8、12、13显示了对人食管癌细胞Ec9706不同程度的抑制活性。
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| 关 键 词： | 合成 氟尿嘧啶 缀合物 抗肿瘤活性 |
| 收稿时间： | 2008-10-30 |
| 修稿时间： | 2009-2-23 |
Synthesis and Cytotoxicity of Derivatives of Fluorouracil Conjugated with Three‐membered Ring |
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| Le WANG,Yunxiao ZHANG,Jingchao TAO.Synthesis and Cytotoxicity of Derivatives of Fluorouracil Conjugated with Three‐membered Ring[J].Chinese Journal of Chemistry,2009,27(7):1374-1378. |
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| Authors: | Le WANG Yunxiao ZHANG Jingchao TAO |
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| Institution: | New Drug Research & Development Center, Department of Chemistry, Zhengzhou University, Zhengzhou, Henan 450052, China |
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| Abstract: | A novel series of 3‐membered ring fluorouracil conjugates including cyclopropylmethyl fluorouracil and (2,3‐epoxypropyl) fluorouracil conjugates were synthesized via selective protection, and their structures were confirmed by IR, 1H NMR and HRMS. Cytotoxicities in vitro of these conjugates were evaluated. Compounds 7 , 8 , 12 and 13 have shown cytotoxicities against Ec9706 cells in different degrees. |
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| Keywords: | synthesis 5‐fluorouracil conjugate cytotoxicity |
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