四种5-氟尿嘧啶二肽衍生物的合成、晶体结构和抗癌活性

Synthesis, Crystal Structure and Anticarcinogenic Activity of Four 5-Fluorouracil-dipeptide Derivatives

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13CNMR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.

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.