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

Synthesis and Bioevaluation of 5-Fluorouracil Derivatives

1email, 2, 2email, 3, 1 and 3,* email
Received: 9 August 2007; in revised form: 9 October 2007 / Accepted: 9 October 2007 / Published: 6 November 2007
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: 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
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MDPI and ACS Style

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.

AMA Style

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(11):2450-2457.

Chicago/Turabian Style

Tian, Zhi-Yong; Du, Gang-Jun; Xie, Song-Qiang; Zhao, Jin; Gao, Wen-Yuan; Wang, Chao-Jie. 2007. "Synthesis and Bioevaluation of 5-Fluorouracil Derivatives." Molecules 12, no. 11: 2450-2457.

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