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• Xiong, J
• Zhu, H
• Zhao, Y
• Lan, Y
• Jiang, J
• Yang, J
• Zhang, S
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• Xiong, J
• Zhu, H
• Zhao, Y
• Lan, Y
• Jiang, J
• Yang, J
• Zhang, S
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• Xiong, J
• Zhu, H
• Zhao, Y
• Lan, Y
• Jiang, J
• Yang, J
• Zhang, S

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Molecules 2009, 14(9), 3142-3152; doi:10.3390/molecules14093142

Article

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

Jing Xiong ^1,2,* , Hai-Feng Zhu ¹ , Ya-Juan Zhao ¹ , Yun-Jun Lan ¹ , Ji-Wang Jiang ¹ , Jing-Jing Yang ²  and Shu-Feng Zhang ^2,*

¹ College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325000, China ² 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

Download PDF Full-Text [217 KB, uploaded 24 August 2009 19:00 CEST]

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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