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一种在晚期小鼠白血病中具有增强活性的新型甾体烷基化剂。

A new steroidal alkylating agent with improved activity in advanced murine leukemias.

作者信息

Catsoulacos P, Politis D, Wampler G L

出版信息

Cancer Chemother Pharmacol. 1979;3(1):67-70. doi: 10.1007/BF00254423.

Abstract

The homo-aza-steroidal ester of [p-[bis(2-chloroethyl)amino]phenoxy] acetic acid, 3 beta-hydroxy 13 alpha - amino - 13,17 - seco - 5 alpha-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl)aminophenoxyacetate, gave a 100% increase in lifespan over controls in the treatment of L1210 leukemia by IP administration on a days 1 and 4 treatment schedule. This ester gave a maximum activity of 383% increased lifespan over controls in the treatment of P388 leukemia by IP administration on a daily treatment schedule. Activity in advanced L1210 (41% increased lifespan) and P388 leukemias (173% increased lifespan) was maintained, indicating that this compound is the most promising of a number of congeners tested to date.

摘要

[对-[双(2-氯乙基)氨基]苯氧基]乙酸的高氮杂甾体酯,即3β-羟基-13α-氨基-13,17-开环-5α-雄甾烷-17-酸-13,17-内酰胺-p-双(2-氯乙基)氨基苯氧基乙酸酯,在第1天和第4天腹腔注射给药治疗L1210白血病时,其寿命比对照组延长了100%。该酯在每日腹腔注射给药治疗P388白血病时,寿命比对照组延长了383%,达到最大活性。在晚期L1210白血病(寿命延长41%)和P388白血病(寿命延长173%)中也保持了活性,表明该化合物是迄今为止测试的众多同系物中最有前景的。

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