Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil

作者：Jing Xiong, Haifeng Zhu, Yajuan Zhao, Lan Yun-jun, Jiwang Jiang, Jingjing Yang, Shufeng Zhang · 发表于：Molecules · 年份：2009 · DOI：10.3390/molecules14093142 · 被引用次数：28 · 研究领域：Cancer therapeutics and mechanisms、Synthesis and biological activity、Synthesis and Biological Evaluation

A series of amino acid ester derivatives containing 5-fluorouracil were synthesized using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC*HCl) and N-hydroxybenzotriazole (HOBt) as a coupling agent. The structures of the products were assigned by NMR, MS, IR etc. The in vitro antitumor activity tests against leukaemia HL-60 and liver cancer BEL-7402 indicated that (R)-ethyl 2-(2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamido)-3-(4-hydroxyphenyl) propanoate showed more inhibitory effect against BEL-7402 than 5-FU.