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新型环氧化合物衍生物抗肿瘤活性的临床前评估

Preclinical evaluation of the anti tumour activity of new epoxyde derivatives.

作者信息

Atassi G, Dumont P, Fisher U, Zeidler M, Budnowski M

出版信息

Cancer Treat Rev. 1984 Mar;11 Suppl A:99-110. doi: 10.1016/0305-7372(84)90048-3.

Abstract

As a follow-up to our initial results on the antineoplastic activity of alpha-1,3,5-triglycidyl-s-triazinetrione (alpha TGT, NSC-296934, Teroxirone), many new epoxyde derivatives were tested against murine tumours, mostly against P388 leukaemia, to determine their antineoplastic role and to characterize their specific effect against tumour cells in vivo, as well as to select an analogue with higher anti-cancer properties and superior pharmacological properties. Triglycidyl urazol (TGU, NSC-332488) showed the highest therapeutic activity and a good level of water-solubility which makes this agent a good candidate for phase-one clinical trials.

摘要

作为我们关于α-1,3,5-三缩水甘油基-s-三嗪三酮(αTGT,NSC-296934,替洛昔隆)抗肿瘤活性初步结果的后续研究,我们对许多新的环氧化物衍生物进行了针对小鼠肿瘤的测试,主要是针对P388白血病,以确定它们的抗肿瘤作用,表征它们在体内对肿瘤细胞的特定效应,并选择一种具有更高抗癌特性和卓越药理特性的类似物。三缩水甘油基乌拉唑(TGU,NSC-332488)表现出最高的治疗活性和良好的水溶性,这使得该药物成为一期临床试验的良好候选药物。

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