Studies on Fluorinated Pyrimidines. II. Synthesis and Antitumor Activity of 5-Fluoro-6-substituted-5, 6-dihydrouracil-5-carboxylic Acid Derivatives

Abstract

Various derivatives of 5-fluoro-5, 6-dihydrouracil with an alkoxycarbonyl, substituted carbamoyl, or cyano group at C-5, and one of a variety of substituents, i.e., alkoxy, substituted mercapto, substituted amino, acyl amino, and alkylidene- and arylideneaminooxy at C-6, have been synthesized as a class of potential pro-drugs of autitumor agents, 5-fluorouracil (5-FU) and 1-(2-tetrahydrofuryl)-5-fluorouracil (Ftorafur). Antitumor activity of these compounds against leukemia P388 or L1210 in mice and antifungal activity against Botrytis cinerea are described.