磷氮化合物。21. 金刚烷基氮丙啶化合物的小鼠溶瘤和抗生育作用。

Phosphorus-nitrogen compounds. 21. Murine oncolytic and antifertility effect of adamantylaziridine compounds.

作者信息

Cates L A, Cramer M B, Williams L

出版信息

J Med Chem. 1978 Jan;21(1):143-6. doi: 10.1021/jm00199a032.

PMID:619145

Abstract

P,P-Bis(1-aziridinyl)-N-adamantylphosphinic amide and N,N'-bis(ethylene)-P-(1-adamantyl)phosphonic diamide were synthesized as potential anticancer and male antifertility agents. Log P values (octanol-water) of the agents were determined and compared to calculated values. Both derivatives displayed intraperitoneal murine antileukemic activity and antifertility effects when given intraperitoneally and orally.

摘要

合成了P,P-双(1-氮丙啶基)-N-金刚烷基次膦酰胺和N,N'-双(亚乙基)-P-(1-金刚烷基)膦酸二酰胺作为潜在的抗癌和男性抗生育剂。测定了这些药剂的log P值（正辛醇-水）并与计算值进行比较。当通过腹腔注射和口服给药时，这两种衍生物均显示出腹腔内小鼠抗白血病活性和抗生育作用。