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Molecules 2007, 12(11), 2450-2457; doi:10.3390/12112450

Synthesis and Bioevaluation of 5-Fluorouracil Derivatives

2, 2
3, 1 and 3,*
1 School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, 300072, Tianjin, P. R. China 2 College of Pharmaceutical Science, Henan University, Jinming District, 475001, Kaifeng, Henan, P. R. China 3 Institute of Natural Products and Medicinal Chemistry, College of Chemistry and Chemical Engineering, Henan University, Jinming District, 475001, Kaifeng, Henan, P. R. China
* Author to whom correspondence should be addressed.
Received: 9 August 2007 / Revised: 9 October 2007 / Accepted: 9 October 2007 / Published: 6 November 2007
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A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and theirstructures confirmed by 1H- and 13C-NMR, MS and elemental analysis. The preliminary invitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions ofliver cancer H22 demonstrated that some of these compounds effectively inhibit the growthof tumor cells, but the in vivo trials in mice revealed that the compounds also exhibitedserious liver and lung tissue toxicity. The hydrolysis experiments indicated that this type ofcompound did not readily liberate 5-fluorouracil, as expected.
Keywords: 5-Fluorouracil; prodrug; synthesis; bioevaluation 5-Fluorouracil; prodrug; synthesis; bioevaluation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Tian, Z.-Y.; Du, G.-J.; Xie, S.-Q.; Zhao, J.; Gao, W.-Y.; Wang, C.-J. Synthesis and Bioevaluation of 5-Fluorouracil Derivatives. Molecules 2007, 12, 2450-2457.

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