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Molecules 2009, 14(9), 3142-3152;

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

College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325000, China
State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012, China
Authors to whom correspondence should be addressed.
Received: 15 July 2009 / Revised: 18 August 2009 / Accepted: 20 August 2009 / Published: 25 August 2009
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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.
Keywords: 5-fluorouracil; amino acid ester; antitumor activity 5-fluorouracil; amino acid ester; antitumor activity

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Xiong, J.; Zhu, H.-F.; Zhao, Y.-J.; Lan, Y.-J.; Jiang, J.-W.; Yang, J.-J.; Zhang, S.-F. Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil. Molecules 2009, 14, 3142-3152.

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