肿瘤抑制性三氮烯。2. 同系物系列中抗肿瘤活性的变化。
Tumor inhibitory triazenes. 2. Variation of antitumor activity within an homologous series.
作者信息
Wilman D E, Goddard P M
出版信息
J Med Chem. 1980 Sep;23(9):1052-4. doi: 10.1021/jm00183a017.
PMID:7411549
Abstract
An homologous series of water-soluble, chemically stable analogues of 5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide (DTIC) has been prepared with activity comparable to DTIC in an experimental tumor system. The antitumor activity of this series of 3-alkyl-1-(4-carboxyphenyl)-3-methyltriazenes rapidly diminishes at alkyl chain lengths greater than pentyl. Partition coefficients were determined, but no relationship between these and antitumor activity could be established.
摘要
已制备出一系列5-(3,3-二甲基-1-三氮烯基)咪唑-4-甲酰胺（DTIC）的水溶性、化学稳定类似物，其在实验肿瘤系统中的活性与DTIC相当。该系列3-烷基-1-(4-羧基苯基)-3-甲基三氮烯的抗肿瘤活性在烷基链长度大于戊基时迅速降低。测定了分配系数，但未能确定其与抗肿瘤活性之间的关系。
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