Two macrocyclic 1,2,3-triazolyl uridine analogues were obtained for the first time by a copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. A 29-membered macrocycle consisted of one uracil molecule, two D-ribofuranose molecules and four 1,2,3-triazole molecules. A 58-membered macrocycle consisted of two uracil mol-ecules, four D-ribofuranose molecules and eight 1,2,3-triazole molecules. Both macro cycles demonstrated moderate cytotoxicity against eight human cancer cell lines and normal cell line WI-38.