Abstract: AimTo synthesize the selenophosphocholine analogues containing tegafur and test their antitumor activities. MethodsThe cyclic glyceroselenophospholopid conjugate of tegafur was synthesized by the reaction of hexaethylphosphorous triamide with N¹-(2-furanidyl)-N³-(hydroxyalkyl)-5-fluyorouracil and 1-O-hexadecyl glycerol as well as selenium in one-pot. Cyclic glyceroselenophospholopid conjugate of tegafur reacted with triethylamine to give title compounds. ResultsSix new compounds have been synthesized. Their structures were confirmed by ¹H NMR, 13P NMR and elemental analysis. Antitumor activity of the title compounds against PGA₁ was tested. ConclusionThe reaction of triethylamine with cyclic glyceroselenophospholopid conjugate of tegafur very readily occurred, which was finished within 2 h at room temperature. The opening-ring products of trans isomers showed antimutor activity against human uriaryl bladder cancer cell more effective than that of the tegafur.