Madelmont J C, Godeneche D, Parry D, Duprat J, Chabard J L, Plagne R, Mathe G, Meyniel G
J Med Chem. 1985 Sep;28(9):1346-50. doi: 10.1021/jm00147a040.
Three chemical pathways were used for the synthesis of four new N'-(2-chloroethyl)-N-[2-(methylsulfinyl)ethyl]- and N'-(2-chloroethyl)-N-[2-(methylsulfonyl)ethyl]-N- or N'-nitrosoureas. These compounds are plasma metabolites of CNCC, a promising antineoplastic (2-chloroethyl)nitrosourea. Preliminary antitumor evaluation was performed against L1210 leukemia implanted intraperitoneally in mice. Among these compounds, two of them exhibited a greater antitumor activity compared to that of the parent mixture.
采用三种化学途径合成了四种新型的N'-(2-氯乙基)-N-[2-(甲基亚磺酰基)乙基]-和N'-(2-氯乙基)-N-[2-(甲基磺酰基)乙基]-N-或N'-亚硝基脲。这些化合物是CNCC的血浆代谢产物,CNCC是一种有前景的抗肿瘤(2-氯乙基)亚硝基脲。对腹腔接种L1210白血病的小鼠进行了初步抗肿瘤评估。在这些化合物中,其中两种表现出比母体混合物更强的抗肿瘤活性。