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. 2009 Aug 25;14(9):3142-52.
doi: 10.3390/molecules14093142.

Synthesis and antitumor activity of amino acid ester derivatives containing 5-fluorouracil

Jing Xiong  1 , Hai-Feng Zhu, Ya-Juan Zhao, Yun-Jun Lan, Ji-Wang Jiang, Jing-Jing Yang, Shu-Feng Zhang
Affiliations

Synthesis and antitumor activity of amino acid ester derivatives containing 5-fluorouracil

Jing Xiong et al. Molecules. .

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.

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Figures

Scheme 1
Scheme 1
Synthesis of 2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-aceto amino acid ester derivatives 2.
Figure 1
Figure 1
Structural formulae of compounds 2.
See this image and copyright information in PMC

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