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

…, PM Goddard, LI Hart, K Merai, DR Newell

Index: Wilman, Derry E. V.; Cox, Peter J.; Goddard, Phyllis M.; Hart, Leigh I.; Merai, Kanti; Newell, David R. Journal of Medicinal Chemistry, 1984 , vol. 27, # 7 p. 870 - 874

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Citation Number: 20

Abstract

The in vivo antitumor activity and in vitro metabolic dealkylation have been measured for an homologous series of 3-alkyl-l-(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 ...