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本文报道一系列含硫亚硝基脲衍生物的合成、光谱学特征及对小鼠白血病L1210的作用。这些化合物都是CNC-半胱胺的衍生物,包括二硫化合物、2-氯乙基氨甲酸酯衍生物以及与羰基化合物环合而成的2,2-二取代的CNC-四氢噻唑。CNC-半胱胺及其二硫化合物、CNC-胱胺甲酰叠氮均有良好的抗L1210的作用;相应的氨甲酸酯衍生物和四氢噻唑衍生物的作用不明显。值得注意的是,2-甲基-2-乙氧羰甲基-3-CNC-四氢噻唑(15b)是一个例外,它对L1210有显著的抑制作用。
This article reports the synthesis, spectroscopic characterization of a series of sulfur-containing nitrosourea derivatives and their effect on murine leukemia L1210. These compounds are derivatives of CNC-Cysteamine, including disulfides, 2-chloroethylcarbamate derivatives and 2,2-disubstituted CNC-tetrahydrothiazoles cyclized with carbonyl compounds . CNC-Cysteamine and its disulfide compounds, CNC cystamine azide have a good anti-L1210 role; the corresponding carbamate derivatives and tetrahydrothiazole derivatives role is not obvious. It is noteworthy that 2-methyl-2-ethoxycarbonylmethyl-3-CNC-tetrahydrothiazole (15b) is an exception which has a significant inhibitory effect on L1210.