N-methylformamide: antitumour activity and metabolism in mice.
The antitumour activities of N-methylformamide, N-ethylformamide and formamide against a number of murine tumours in vivo (Sarcoma 180, M5076 ovarian sarcoma and TLX5 lymphoma) have been estimated. In all cases N-methyl-formamide had significant activity, formamide had marginal or no activity and N-ethylformamide had no significant activity. N-methylformamide and N-ethylformamide were equitoxic to the TLX5 lymphoma in vitro. Formamide was found as a metabolite in the plasma and urine of animals given N-methylformamide and N-ethylformamide, but excretion profiles do not support the hypothesis that formamide is an active antitumour species formed from N-alkylformamides. No appreciable metabolism of N-methylformamide occurred under a variety of conditions with liver preparations in vitro. N-methylformamide, but not N-ethylformamide or formamide, reduced liver soluble non-protein thiols by 59.8% 1 h after administration of an effective antitumour dose.
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism / Q000627:therapeutic use*; D005260:Female; D005559:Formamides / Q000378:metabolism / Q000627:therapeutic use*; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D008223:Lymphoma / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008808:Mice, Inbred CBA; D009374:Neoplasms, Experimental / Q000188:drug therapy; D010051:Ovarian Neoplasms / Q000188:drug therapy; D012513:Sarcoma, Experimental / Q000188:drug therapy*; D013438:Sulfhydryl Compounds / Q000378:metabolism
D000970:Antineoplastic Agents; D005559:Formamides; D013438:Sulfhydryl Compounds; C035404:N-ethylformamide; C002950:methylformamide