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 [a]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.

Key words: 5-fluorouracil-dipeptide derivative, crystal structure, enantiomer, anticarcinogenic activity, cyclic voltammogram