摘要
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).
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1995年第6期896-899,共4页
Chemical Journal of Chinese Universities
基金
国家自然科学基金