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

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

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 antitum...

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Main Authors: Jing Xiong, Hai-Feng Zhu, Ya-Juan Zhao, Yun-Jun Lan, Ji-Wang Jiang, Jing-Jing Yang, Shu-Feng Zhang
Format: Article
Language:English
Published: MDPI AG 2009-08-01
Series:Molecules
Subjects:
5-fluorouracil
amino acid ester
antitumor activity
Online Access:http://www.mdpi.com/1420-3049/14/9/3142/
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spelling doaj-0cdebc2a079a4f7388a9b1e4749ea3282020-11-24T22:04:50ZengMDPI AGMolecules1420-30492009-08-011493142315210.3390/molecules14093142Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-FluorouracilJing XiongHai-Feng ZhuYa-Juan ZhaoYun-Jun LanJi-Wang JiangJing-Jing YangShu-Feng ZhangA 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. http://www.mdpi.com/1420-3049/14/9/3142/5-fluorouracilamino acid esterantitumor activity
collection DOAJ
language English
format Article
sources DOAJ
author Jing Xiong
Hai-Feng Zhu
Ya-Juan Zhao
Yun-Jun Lan
Ji-Wang Jiang
Jing-Jing Yang
Shu-Feng Zhang
spellingShingle Jing Xiong
Hai-Feng Zhu
Ya-Juan Zhao
Yun-Jun Lan
Ji-Wang Jiang
Jing-Jing Yang
Shu-Feng Zhang
Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
Molecules
5-fluorouracil
amino acid ester
antitumor activity
author_facet Jing Xiong
Hai-Feng Zhu
Ya-Juan Zhao
Yun-Jun Lan
Ji-Wang Jiang
Jing-Jing Yang
Shu-Feng Zhang
author_sort Jing Xiong
title Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
title_short Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
title_full Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
title_fullStr Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
title_full_unstemmed Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil
title_sort synthesis and antitumor activity of amino acid ester derivatives containing 5-fluorouracil
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2009-08-01
description 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.
topic 5-fluorouracil
amino acid ester
antitumor activity
url http://www.mdpi.com/1420-3049/14/9/3142/
work_keys_str_mv AT jingxiong synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT haifengzhu synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT yajuanzhao synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT yunjunlan synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT jiwangjiang synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT jingjingyang synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
AT shufengzhang synthesisandantitumoractivityofaminoacidesterderivativescontaining5fluorouracil
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