Mutagenicity of anti-cancer nitrobenzofuroxans.
Anti-leukaemically active benzofuroxans were tested for mutagenicity in Salmonella typhimurium. Mutagenicity was not found to be correlated to the previously established anti-leukaemic activity. One anti-leukaemically inactive compound after exposure to liver microsomal enzymes proved the most mutagenic of the derivatives for TA100, whereas after similar treatment, the mutagenicity of the most potent anti-leukaemic compound was reduced. All twelve derivatives tested were mutagenic in a base-substitution strain which was defective in excision-repair and also carried a plasmid-linked repair deficiency. Mutagenicity of five dervatives was undetectable in strains proficient for one or the other of the above repair pathways. Nine of the benzofuroxans could also be detected as mutagens in the frameshift tester strain TA98.
D000818:Animals; D004260:DNA Repair; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism; D009153:Mutagens; D009578:Nitrobenzenes / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D010069:Oxadiazoles / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D010957:Plasmids; D012486:Salmonella typhimurium / Q000187:drug effects*; D013329:Structure-Activity Relationship
D009153:Mutagens; D009578:Nitrobenzenes; D010069:Oxadiazoles; C014701:nitrobenzofuroxan