Synthesis and Bioevaluation of 5-Fluorouracil Derivatives

Molecules

Zhi-Yong Tian³  Gang-Jun Du²  Song-Qiang Xie²  Jin Zhao¹  Wen-Yuan Gao³ 

[1] Institute of Natural Products and Medicinal Chemistry, College of Chemistry and Chemical Engineering, Henan University, Jinming District, 475001, Kaifeng, Henan, P. R. China;College of Pharmaceutical Science, Henan University, Jinming District, 475001, Kaifeng, Henan, P. R. China; Phone: [phone]; E-mail:;School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, 300072, Tianjin, P. R. China; Phone: [phone]; E-mail:

关键词: 5-Fluorouracil;    prodrug;    synthesis;    bioevaluation;   

DOI  :  10.3390/12112450

来源: mdpi

【 摘 要 】

A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and their structures confirmed by ¹H- and ¹³C-NMR, MS and elemental analysis. The preliminary in vitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions of liver cancer H₂₂ demonstrated that some of these compounds effectively inhibit the growth of tumor cells, but the in vivo trials in mice revealed that the compounds also exhibited serious liver and lung tissue toxicity. The hydrolysis experiments indicated that this type of compound did not readily liberate 5-fluorouracil, as expected.

【 授权许可】

Unknown   
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