Foye W O, Lowe Y H, Lanzillo J J
J Pharm Sci. 1976 Aug;65(8):1247-51. doi: 10.1002/jps.2600650830.
A series of N-heterocyclic and N-heterocyclic alkyl derivatives of bis(2-aminoethyl) disulfide and aminoethanethiosulfuric acid was synthesized as potential antiradiation and anticancer agents. The compounds were prepared by the reactions of the heterocyclic halides with bis(2-aminoethyl) disulfide and aminoethanethiosulfuric acid. A dithio acid derivative, 3,3-dimercapto-2-cyanoacryloylpyrrolidide, was also prepared. Several compounds, including the dithio acid derivative, provided good radiation protection to mice. None of the compounds screened showed appreciable anticancer activities in two leukemia systems.
合成了一系列双(2-氨基乙基)二硫化物和氨基乙硫代硫酸的N-杂环及N-杂环烷基衍生物,作为潜在的抗辐射和抗癌剂。这些化合物是通过杂环卤化物与双(2-氨基乙基)二硫化物和氨基乙硫代硫酸反应制备的。还制备了一种二硫代酸衍生物,3,3-二巯基-2-氰基丙烯酰吡咯烷。包括二硫代酸衍生物在内的几种化合物对小鼠具有良好的辐射防护作用。在两个白血病系统中,所筛选的化合物均未显示出明显的抗癌活性。