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

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.

• Authors: D E Wilman, P J Cox, P M Goddard, L I Hart, K Merai, D R Newell
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 27 Issue 7 Pg. 870-4 (Jul 1984) ISSN: 0022-2623 [Print] United States
• PMID: 6737430 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Triazenes

Topics

• Animals
• Antineoplastic Agents (chemical synthesis)
• Chromatography, High Pressure Liquid
• Female
• Lymphoma (drug therapy)
• Mathematics
• Mice
• Mice, Inbred CBA
• Microsomes, Liver (metabolism)
• Structure-Activity Relationship
• Triazenes (chemical synthesis, therapeutic use)