Abdaoui M, Dewynter G, Aouf N, Favre G, Morère A, Montero J L
Laboratoire de Chimie Biomoléculaire (assoc. CNRS), Université de Montpellier-II, France.
Bioorg Med Chem. 1996 Aug;4(8):1227-35. doi: 10.1016/0968-0896(96)00118-6.
A new series of alkylating agents, 2-chloroethylnitrososulfamides (CENS), were developed on the model of 2-chloroethylnitrosoureas. Starting from chlorosulfonyl isocyanate, a four-step synthesis (carbamoylation-sulfamoylation, Mitsunobu alkylation, deprotection, and nitrosation) gives the title compounds in a 47-58% overall yield. The selection of the nitrosation site can be directed through an alternative route. The pharmacological evaluation shows a significant oncostatic activity towards both A549 and MCF7 cell lines.
基于2-氯乙基亚硝基脲模型开发了一系列新型烷基化剂,即2-氯乙基亚硝基磺酰胺(CENS)。以氯磺酰异氰酸酯为起始原料,经过四步合成(氨甲酰化-氨磺酰化、光延烷基化、脱保护和亚硝化),以47%-58%的总收率得到目标化合物。亚硝化位点的选择可以通过另一条路线进行引导。药理评价表明,该化合物对A549和MCF7细胞系均具有显著的抑癌活性。