Journal of Chinese Pharmaceutical Sciences ›› 2021, Vol. 30 ›› Issue (9): 743-753.DOI: 10.5246/jcps.2021.09.062

• Original articles • Previous Articles     Next Articles

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

Shiqi Xu1, Liyan Zhu1, Chao Hao1, Wenqian Liu1, Chenglong Chen2, Yongyi Chen1, Aiqin Liu1,*()   

  1. 1 Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan 250062, Shandong, China
    2 School of Pharmacy, Shandong University?of?Traditional?Chinese?Medicine, Jinan 250355, Shandong, China
  • Received:2021-04-23 Revised:2021-07-02 Accepted:2021-08-11 Online:2021-09-27 Published:2021-09-27
  • Contact: Aiqin Liu


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.

Key words: Tegafur, 5-Fluorouracil, Amino acid ester, Synthesis, Evaluation, Antitumor activity