Microsomal metabolism of quinifuryl - a nitrofuryl-ethenyl-quinolone antiseptic possessing antitumor activity in vitro

Quinifuryl, 2-(5'-nitro-2'-furanyl)ethenyl-4-{N-[4'-(N,N-dimethylamino)-1'- methylbutyl] carbamoyl} quinoline, is a representative of a family of nitro furan-ethenyl-quinoline antibiotics synthesized in the USSR by Dr N.M. Sukh ova. The drug has been shown to be an effective cytostatic and radiosensiti zer towards cancer cells in culture. While rapid metabolic consumption of t hese drugs by liver tissue has been shown, none of the drug metabolites hav e been isolated and characterized. Here, we present the results of experime nts focusing on the isolation and characterization of quinifuryl metabolite s. A pyridine derivative was the sole product detected and characterized by GC-MS analysis. An alteration of quinifuryl metabolism by peroxynitrite fo rmed during the metabolism of the drug was assumed to be responsible for an unexpectedly high drug decomposition.