肿瘤抑制性三氮烯。3. 同系物中的脱烷基化及其与抗肿瘤活性的关系。

Tumor inhibitory triazenes. 3. Dealkylation within an homologous series and its relation to antitumor activity.

作者信息

Wilman D E, Cox P J, Goddard P M, Hart L I, Merai K, Newell D R

出版信息

J Med Chem. 1984 Jul;27(7):870-4. doi: 10.1021/jm00373a011.

DOI:10.1021/jm00373a011

Abstract

The in vivo antitumor activity and in vitro metabolic dealkylation have been measured for an homologous series of 3-alkyl-1-(4-carbamoylphenyl)-3-methyltriazenes and have been compared with their partition coefficients. This investigation has shown that the extent of oxidative metabolism in vitro and the antitumor activity in vivo of these compounds are dependent upon hydrophobicity. These findings provide confirmation for the relationship between metabolism and antitumor activity for aryldialkyltriazenes.

摘要

已测定了一系列3-烷基-1-(4-氨甲酰基苯基)-3-甲基三氮烯的体内抗肿瘤活性和体外代谢脱烷基作用，并将其与它们的分配系数进行了比较。该研究表明，这些化合物的体外氧化代谢程度和体内抗肿瘤活性取决于疏水性。这些发现证实了芳基二烷基三氮烯的代谢与抗肿瘤活性之间的关系。

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Tumor inhibitory triazenes. 3. Dealkylation within an homologous series and its relation to antitumor activity.肿瘤抑制性三氮烯。3. 同系物中的脱烷基化及其与抗肿瘤活性的关系。

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