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 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.
College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325000, China. xiongjing@wzu.edu.cn
Jing
J
Xiong
Hai-Feng
HF
Zhu
Ya-Juan
YJ
Zhao
Yun-Jun
YJ
Lan
Ji-Wang
JW
Jiang
Jing-Jing
JJ
Yang
Shu-Feng
SF
Zhang
D000596:Amino Acids / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004952:Esters / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005472:Fluorouracil / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans
D000596:Amino Acids; D000970:Antineoplastic Agents; D004952:Esters; D005472:Fluorouracil