Syntheses and Antitumor Activities of New Spin-labeled 5-Fluorouracil Derivatives(Ⅲ)

Chem. J. Chinese Universities ›› 1995, Vol. 16 ›› Issue (6): 896.

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Syntheses and Antitumor Activities of New Spin-labeled 5-Fluorouracil Derivatives(Ⅲ)

WANG Yan-Guang¹, CHEN Yao-Zu¹, XIAO Xin-Liang², LIU Rui-Xian²

1. Department of Chemistry Zhejiang University Hangzhou 310027;
2. Department of Chemistry Tianjin University

Received:1994-06-23 Revised:1995-01-28 Online:1995-06-24 Published:1995-06-24

Abstract

Abstract: Nine new spin-labeled derivatives of 5-fluorouracil,2,5_a-cand 7_a-c,were synthesized and their structures were confirmed by IR,UV,MS and ESR spectra as well as elementary analysis.The antitumor activities of compounds 2 and 5_a-ewere tested against S180 and EAC in mice.The preliminary results showed that the antitumor activities of compound 5_ewas similar to that of 5-fluorouracil, while the acute toxicity of 5_c(LD₅₀=944.8my/kg)was about 8 times lower than that of 5-fluorouracil(LD₅₀=117.2mg/kg).

Key words: Fluorouracil, Spin label, Nitroxyl, Antitumor activity

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WANG Yan-Guang, CHEN Yao-Zu, XIAO Xin-Liang, LIU Rui-Xian. Syntheses and Antitumor Activities of New Spin-labeled 5-Fluorouracil Derivatives(Ⅲ)[J]. Chem. J. Chinese Universities, 1995, 16(6): 896.

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Syntheses and Antitumor Activities of New Spin-labeled 5-Fluorouracil Derivatives(Ⅲ)

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