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Triazene metabolism 3. in vitro cyto toxicity towards m 21 cells and in vivo anti tumor activity of the proposed metabolites of the anti tumor 1 aryl 3 3 dimethyl triazenes



Triazene metabolism 3. in vitro cyto toxicity towards m 21 cells and in vivo anti tumor activity of the proposed metabolites of the anti tumor 1 aryl 3 3 dimethyl triazenes



Canadian Journal of Physiology and Pharmacology 62(4): 396-402



In vitro cytotoxicity of a series of antitumor triazenes towards the M21 [human] melanoma cell line was studied. Dimethyltriazenes are structural analogues of 5-(3,3-dimethyl-1-triazeno-)imidazole-4-carboxamide (dacarbazine) and are inactive, which is consistent with the requirement for metabolic activation. Monomethyltriazenes and hydroxymethyltriazenes, the proposed metabolites of the dimethyltriazenes, are cytotoxic to the M21 cell line. A new series of 4-hydroxy-1,2,3-benzotriazines was tested for in vitro cytotoxicity. A series of monoalkyltriazenes (Ar.cntdot.N .dbd. NHR) was tested for antitumor activity against the P388 [mouse] lymphoma in vivo. Only monomethyltriazenes had significantly antitumor activity, which supports the hypothesis that the monomethyltriazene is the active metabolite of the antitumor dimethyltriazenes. The activity of monomethyltriazenes in vivo is correlated with the chemical stability and t1/2 [half-life] measurements in pH 7.5 phosphate buffer.

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