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synthesis and antitumor activity of amino acid ester derivatives containing 5-fluorouracil合成与抗肿瘤活性氨基酸酯衍生品包含5 -氟尿嘧啶.pdf

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synthesis and antitumor activity of amino acid ester derivatives containing 5-fluorouracil合成与抗肿瘤活性氨基酸酯衍生品包含5 -氟尿嘧啶

Molecules 2009, 14, 3142-3152; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules 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 * Author to whom correspondence should be addressed; E-mails: xiongjing@ (J.X.), Zhangshf@ (S.-F.Z.); Tel.: +86 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 1. Introduction 5-Fluorouracil (5-FU) is an antimetabolite of the pyrimidine analogue type,