Draeger J, Peter G, Hohorst H J
Cancer Treat Rep. 1976 Apr;60(4):355-9.
The reaction of 4-hydroxycyclophosphamide (4-hydroxy-CP) with sulfhydryl (SH) compounds was studied, and although the cytotoxic activity was lost a significant stabilization of the alkylating capacity was observed at the same time. We were able to show that the reaction of 4-hydroxy-CP with thiols lead to an equilibrium between the reaction product and the starting substrates. On the basis of this equilibrium the increased stabilization of the alkylating capacity of the 4-hydroxy-CP derivatives by raising the SH concentration can be explained. The different degrees of stabilization depending on the structure of the thiol results from different equilibria. the effect on the toxification reaction resulting from this equilibrium, in connection with the tautomeric equilibrium between 4-hydroxy-CP and aldophosphamide, is discussed.
研究了4-羟基环磷酰胺（4-hydroxy-CP）与巯基（SH）化合物的反应，虽然细胞毒性活性丧失，但同时观察到烷基化能力有显著的稳定作用。我们能够证明4-羟基-CP与硫醇的反应导致反应产物与起始底物之间达到平衡。基于这种平衡，可以解释通过提高SH浓度来增强4-羟基-CP衍生物烷基化能力的稳定性。取决于硫醇结构的不同程度的稳定性源于不同的平衡。讨论了这种平衡对毒化反应的影响，以及与4-羟基-CP和醛磷酰胺之间互变异构平衡的关系。
