Synthesis of a novel series of amino acid prodrugs based on tegafur and evaluation of their antitumor activity

As an oral chemotherapy prodrug, tegafur, can be converted to 5-fluorouracil, which is activated to kill tumor cells mainly by the inhibition of thymidylate synthase. In the present study, we synthesized 20 new tegafur derivatives containing amino acid ester groups by substitution, hydrolysis, and condensation. Their structures were confirmed by ¹H NMR, ¹³C NMR, and H RMS, and their inhibitory effects on tumor cell growth were studied. The results showed that some of the compounds had good anti-tumor activity.