Voelcker G, Hohorst H J
Zentrum der Biologischen Chemie der Johann Wolfgang Goethe-Universität, Frankfurt am Main, Germany.
J Cancer Res Clin Oncol. 1998;124(6):297-300. doi: 10.1007/s004320050172.
Structure/activity studies were carried out with thiazolidinyl- and perhydrothiazinylphosphamide ester, which differ in the structure of the phosphamide moiety and in the rate of spontaneous hydrolysis to activated oxazaphosphorines. Antitumour activity in mice with advanced P388 tumours growing subcutaneously was increased 30- to 40-fold when one 2-chloroethyl group in l-aldophosphamide-perhydrothiazine was substituted by a mesylethyl group.
对噻唑烷基亚磷酰胺酯和全氢噻嗪基亚磷酰胺酯进行了结构/活性研究，它们在磷酰胺部分的结构以及自发水解为活性恶唑磷的速率方面存在差异。当1-醛磷酰胺-全氢噻嗪中的一个2-氯乙基被甲磺酰乙基取代时，对皮下生长的晚期P388肿瘤小鼠的抗肿瘤活性提高了30至40倍。
