Comparison of metabolism and activity of an aryldimethyltriazene and an aryldiethyltriazene

P. Farina, L. Torti, R. Urso, J. K. Horton, A. Gescher, M. D'Incalci

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The antitumoral activity and metabolism of l-(4-acetylphenyl)-3,3-dimethyltriazene [pAc-(CH3)2] and 1-(4-acetylphenyl)-3,3-diethyltriazene [pAc-(C2H5)2] were studied in mice. pAc-(CH3)2 showed significant antitumoral activity against M5076 ovarian reticular cell sarcoma, L1210 leukemia, EL 4 lymphoma in mice, but not against Lewis lung carcinoma. pAc-(C2H5)2 was inactive in all these murine tumors and was much more toxic than pAc-(CH3)2. pAc-(CH3)2 and pAc-(C2H5)2 were rapidly metabolized in vitro and in vivo to their respective monoalkyltriazenes and to 4-aminoacetophenone (pAc-NH2). In vitro, 79% of the dimethyltriazene was metabolized to its monomethyl analogue, but only 27% of the diethyltriazene was metabolized to the monoethyltriazene. The monoalkytriazenes were almost completely biotransformed to pAc-NH2 by a 9000 g liver fraction. The metabolic pattern in the in vitro study was comparable to that found in vivo.

Original languageEnglish
Pages (from-to)209-215
Number of pages7
JournalBiochemical Pharmacology
Issue number2
Publication statusPublished - Jan 15 1986

ASJC Scopus subject areas

  • Pharmacology


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