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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; in revised form: 18 August 2009 / Accepted: 20 August 2009 / Published: 25 August 2009
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.
Keywords: 5-fluorouracil; amino acid ester; antitumor activity
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MDPI and ACS Style
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.
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(9):3142-3152.
Xiong, Jing; Zhu, Hai-Feng; Zhao, Ya-Juan; Lan, Yun-Jun; Jiang, Ji-Wang; Yang, Jing-Jing; Zhang, Shu-Feng. 2009. "Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil." Molecules 14, no. 9: 3142-3152.