
Journal of Medicinal Chemistry p. 850 - 853 (1977)
Update date:2022-08-03
Topics:
Giraldi
Nisi
Connors
Goddard
Several 1-aryl-3, 3-dimethyltriazene derivatives have been 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 para position to the triazene function. Three p-sulfamoyl derivatives have also been included and proved to be inactive. Among the carbonyl derivatives compounds 1 and 20, which can be used as reference, cause ILS of about 50%, respectively, at four and three dose levels. Compound 16, the o-nitrophenylhydrazone of the hydrazide 1, is active at all six dose levels studied. The adduct 19, obtained from the same hydrazide and p-nitrobenzaldehyde, is active at four dose levels, and the ILS value at two optimum doses are significantly greater than those caused by compound 1.
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(1977)