Abstract
A number of halomethyl-1,2,3-triazole derivatives have been tested for their effect on ICR Swiss female mice bearing the Ehrlich carcinoma ascites (ECA) tumor. Two of these compounds, namely 4-bromomethyl-1-(2,3,4,6-tetra-0-acetyl-β-D-glucopyranosyl)-1,2,3-triazole and 4-iodomethyl-1-(2,3,4,6-tetra-0-acetyl-β-D-glucopyranosyl)-1,2,3-triazole, referred to here as compounds H and K, respectively, promoted a significant increase in the median survival time (145% and 195%) when injected IP for 9 consecutive days at doses of 75 mg/kg/injection and 100 mg/kg/injection, respectively. DNA synthesis, as measured by (methyl-3H)thymidine incorporation into trichloroacetic acid-precipitated material, was always inhibited by all the triazole derivatives to a greater extent than the incorporation of (5,6-3H)uridine, (5-3H)proline, and (6-3H)-glucose. Moreover, inhibition of DNA synthesis was complete and irreversible following exposure to selected triazole derivatives. Compounds H and K inhibited the incorporation of di(3H)methyl sulfate by ECA cells. In addition, compound K promoted the release of radioactivity associated with trichloroacetic acid-insoluble material coming from (8-3H)guanosine-prelabeled cells. This release of radioactivity did not occur when cells were prelabeled with (methyl-3H)thymidine. It is concluded from these results that these triazole derivatives act as alkylating agents.
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