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四种5-氟尿嘧啶二肽衍生物的合成、晶体结构和抗癌活性
  • 期刊名称:化 学 学 报,66(14): 1693–1699,2008(SCI).
  • 时间:0
  • 分类:O614.121[理学—无机化学;理学—化学] TQ463.54[化学工程—制药化工]
  • 作者机构:[1]温州大学化学与材料工程学院,温州325027
  • 相关基金:国家自然科学基金(No.20571057)和温州市科技计划(No.S20060026)资助项目.
  • 相关项目:5-氟尿嘧啶短肽铽配合物的合成、抗癌活性及其与DNA的作用研究
中文摘要:

合成了四种新的5-氟尿嘧啶(5-Fu)二肽衍生物,它们的结构经过元素分析、IR、^1HNMR和^13C NMR的表征,比旋光度[α]D的测定结果表明了它们之间的对映异构关系,用X射线衍射法测定了其中一对对映异构的晶体结构3a(S)和3b(R),生物活性测试的结果表明这四种化合物都具有一定的抑制活性,并且R型产物比S型产物抑制率高.研究了2a和3a与DNA在Au电极上相互作用的伏安行为,比较了它们跟5-氟尿嘧啶与双链DNA发生相互作用的差别.

英文摘要:

Four new 5-fluorouracil-dipeptide derivatives were synthesized and identified by means of elemental analysis, IR, ^1H NMR and ^13C NMR spectra. The enantiomeric relations of the four isomers are reflected by their specific rotations [α]D data, two of which were determined by single crystal X-ray diffraction analysis. The result of the biological test shows that the four compounds have certain antitumor activities, and the R-isomer exhibites higher antibacterial activity than the S-isomer. The voltammetric behavior of 2a and 3a interacting with dsDNA on an Au electrode was investigated, and the interacting differences between them with 5-florouracil were compared.

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