Synthesis and Bioevaluation of 5-Fluorouracil Derivatives

Abstract

A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and theirstructures confirmed by 1H- and 13C-NMR, MS and elemental analysis. The preliminary invitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions ofliver cancer H22 demonstrated that some of these compounds effectively inhibit the growthof tumor cells, but the in vivo trials in mice revealed that the compounds also exhibitedserious liver and lung tissue toxicity. The hydrolysis experiments indicated that this type ofcompound did not readily liberate 5-fluorouracil, as expected.

Keywords

• 5-Fluorouracil
• prodrug
• synthesis
• bioevaluation