Kutscher B, Niemeyer U, Engel J, Kleemann A, Hilgard P, Pohl J, Scheffler G
ASTA Medica AG, Frankfurt/Main, Fed. Rep. of Germany.
Arzneimittelforschung. 1995 Mar;45(3):323-6.
Two ifosfamide (CAS 3778-73-2) analogs with a five-membered ring, i.e. the oxazaphospholidine derivatives 6 and 7, were synthesized and their cytotoxic activity in vitro, acute toxicity and antitumor activity in vivo determined in comparison with the oxazaphorinane ifosfamide 1. The observed low biological activity gives evidence that both, the six-membered oxazaphosphorinane ring and the two N-2-chloroethyl-side chains are necessary for the generation of the ultimate alkylator, i.e. the ifosfamide mustard 5.
合成了两种具有五元环的异环磷酰胺（CAS 3778-73-2）类似物，即恶唑磷烷衍生物6和7，并与恶唑磷杂环已烷异环磷酰胺1相比，测定了它们的体外细胞毒性活性、急性毒性和体内抗肿瘤活性。观察到的低生物活性表明，六元恶唑磷杂环已烷环和两个N-2-氯乙基侧链对于生成最终烷化剂即异环磷酰胺氮芥5都是必需的。
