Preparation and antitumor activity of 1-aryl-3,3-dimethyltriazene derivatives

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Abstract
Several 1-aryl-3,3-dimethyltriazene derivatives were synthesized and tested for their antitumor activity against the TLX5 lymphoma in mice. These compounds are characterized by the presence of a carbonyl group bound to the benzene nucleus in the p-position to the triazene function. Three p-sulfamoyl derivatives were also included and proved to be inactive. Among the carbonyl derivatives compounds 1 and 20, which can be used as reference, cause ILS of .apprx. 50%, respectively, at 4 and 3 dose levels. Compound 16, the o-nitrophenylhydrazone of the hydrazide 1, is active at all 6 dose levels studied. The adduct 19, obtained from the same hydrazide and p-nitrobenzaldehyde, is active at 4 dose levels, and the ILS values at 2 optimum doses are significantly greater than those caused by compound 1.

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