Studies on the antitumor activity of 1,3-Bis(Tetrahydro-2-Furanyl)-5-Fluoro-2,4-Pyrimidinedione (FD-1), a new antitumor agent. I

Abstract

The antitumor activity of 1,3-Bis (tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione (FD-1) was compared with that of l-(2-Tetrahydrofuryl)-5-fluorouracil (FT) or 5-Fluorouracil (5-FU) in a number of tumor systems. FD-1 had significant activity against the solid forms but not the ascitic forms, and it produced a greater inhibition in tumor growth than FT. On AH 130 solid form, the therapeutic index(LD50/ED50) of FD-1 and FT were respectively 18.3 and 10. 6. FD-1 was evaluated against the ip and sc implanted L1210 leukemia by single, intermittent or daily administration. FD-1 retained some degree of antileukemic activity against the ic implanted L 1210. No significant difference in antitumor activity was observed between the R and S isomers or the racemic mixture (FD-1). A higher activity of FD-1 compared to FT was possibly due to the increased 5-FU level in tumor through its metabolite, 3-(tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione (3-FT). © 1978, Japanese Society of Chemotherapy. All rights reserved.