氟脲嘧啶自旋标记衍生物的合成与抗肿瘤活性（Ⅲ）

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

合成了９个新的５－氟脲嘧啶自旋标记衍生物２、５ａ－ｅ和７ａ－ｃ，经元素分析、ＩＲ、ＵＶ、ＭＳ和ＥＳＲ确定了其组成和结构。对化合物２和５ａ－ｅ进行了抗小鼠艾氏腹水癌和肉瘤Ｓ１８０的体内筛选。初步试验结果表明：化合物５ｃ对两种瘤株均显示较强的抑制作用，其抗肿瘤活性与５－氟脲嘧啶相似，而５ｅ（ＬＤ５０＝９４４．８ｍｙ／ｋｇ）的急性毒性比５－氟脲嘧啶（ＬＤ５０＝１１７．２ｍｇ／ｋｇ）降低约８倍。

Nine new spin-labeled derivatives of 5-fluorouracil,2,5a-cand 7a-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 5a-e were tested against S180 and EAC in mice.The preliminary results showed that the antitumor activities of compound 5e was similar to that of 5-fluorouracil, while the acute toxicity of 5c (LD50=944.8my/kg)was about 8 times lower than that of 5-fluorouracil(LD50=117.2mg/kg).