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

Jing Xiong, Hai-Feng Zhu, Ya-Juan Zhao and 4 more

Molecules · 2009

doi:10.3390/molecules14093142 (opens in a new tab)

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Abstract

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.

Abstract licence: CC BY

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