Mutation Research/Genetic Toxicology and Environmental Mutagenesis, 2002
The mutagenic activity of sulfoscanate (SSC) (4-isothiocyanate-4-nitrodiphenyl sulphide) has been... more The mutagenic activity of sulfoscanate (SSC) (4-isothiocyanate-4-nitrodiphenyl sulphide) has been compared with that of the following reported drugs: (a) nitroscanate (NSC) (4-isothiocyanate-4-nitrodiphenyl ether) which is a veterinary anthelmintic drug and (b) amoscanate (ASC) (4-isothiocyanate-4-nitrodiphenyl amine) which is effective against schistosomes. SSC has been found to be a very potent mutagen towards TA98 and TA100 inducing 26.0 and 475.5 revertants/nmole, respectively. NSC was found to induce mutations at a rate of 11.1 and 21.5 revertants/nmole in TA98 and TA100, respectively. ASC was found to be non-mutagenic as such, but the urine of animals given the drug displayed mutagenicity. When SSC was tested in TA98/1,8-DNP 6 , deficient in O-acetyltransferase, the activity decreased to 10.0 revertants/nmole. However, in case of NSC the mutagenic activity was reduced to 0.24 revertants/nmole, indicating the importance of O-acetyltransferase in generating N-acetoxyarylamine. In TA98NR, deficient in nitroreductase, the mutagenicity of SSC and NSC was totally absent. The positional isomers of SSC, 4-isothiocyanate-3-nitro-and 4-isothiocyanate-2-nitrodiphenyl sulphide, were found to be non-mutagenic in both TA98 and TA100. Our comparison of the mutagenic activity of SSC, NSC and ASC indicates that the pattern of activity is SSC > NSC > ASC.
Mutation Research/Genetic Toxicology and Environmental Mutagenesis, 2001
A variety of nitro-substituted phenyl alkyl/aryl thioethers and nitroso-substituted phenyl alkyl/... more A variety of nitro-substituted phenyl alkyl/aryl thioethers and nitroso-substituted phenyl alkyl/aryl thioethers have been synthesized and tested for their mutagenicity towards Salmonella typhimurium strain TA100, TA98, TA98NR and TA98/1,8-DNP 6 in the absence of S9 mix. The relative order of mutagenicity in TA98 and TA100 among p-nitrophenyl thioethers having alkyl or aryl substituents is allyl > phenyl > benzyl > butyl > propyl > ethyl > methyl. Compounds having an alkyl chain C 6 to C 12 were found to be non-mutagenic. Among the various positional isomers (ortho, meta and para) of nitro-substituted diphenyl thioethers only the compounds having the-NO 2 function at the para position is mutagenic, whereas compounds having a-NO 2 function at ortho and meta are non-mutagenic. However, the reduced intermediate, ortho-nitroso derivative was found to be mutagenic in all the four strains but the meta-nitroso derivative was found to be non-mutagenic. All mutagens were found to be non-mutagenic when tested in nitroreductase deficient strain TA98NR, whereas their nitroso intermediates are found to be mutagenic. A substantial fall in the mutagenic activity is observed when some mutagens are tested in O-acetyltransferase deficient strain TA98/1,8-DNP 6 .
Ortho-, meta-and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and test... more Ortho-, meta-and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and tested for their mutagenicity toward Salmonella typhimurium TA100, TA100NR (nitroreductase deficient
Mutation Research/Genetic Toxicology and Environmental Mutagenesis, 2002
The mutagenic activity of sulfoscanate (SSC) (4-isothiocyanate-4-nitrodiphenyl sulphide) has been... more The mutagenic activity of sulfoscanate (SSC) (4-isothiocyanate-4-nitrodiphenyl sulphide) has been compared with that of the following reported drugs: (a) nitroscanate (NSC) (4-isothiocyanate-4-nitrodiphenyl ether) which is a veterinary anthelmintic drug and (b) amoscanate (ASC) (4-isothiocyanate-4-nitrodiphenyl amine) which is effective against schistosomes. SSC has been found to be a very potent mutagen towards TA98 and TA100 inducing 26.0 and 475.5 revertants/nmole, respectively. NSC was found to induce mutations at a rate of 11.1 and 21.5 revertants/nmole in TA98 and TA100, respectively. ASC was found to be non-mutagenic as such, but the urine of animals given the drug displayed mutagenicity. When SSC was tested in TA98/1,8-DNP 6 , deficient in O-acetyltransferase, the activity decreased to 10.0 revertants/nmole. However, in case of NSC the mutagenic activity was reduced to 0.24 revertants/nmole, indicating the importance of O-acetyltransferase in generating N-acetoxyarylamine. In TA98NR, deficient in nitroreductase, the mutagenicity of SSC and NSC was totally absent. The positional isomers of SSC, 4-isothiocyanate-3-nitro-and 4-isothiocyanate-2-nitrodiphenyl sulphide, were found to be non-mutagenic in both TA98 and TA100. Our comparison of the mutagenic activity of SSC, NSC and ASC indicates that the pattern of activity is SSC > NSC > ASC.
Mutation Research/Genetic Toxicology and Environmental Mutagenesis, 2001
A variety of nitro-substituted phenyl alkyl/aryl thioethers and nitroso-substituted phenyl alkyl/... more A variety of nitro-substituted phenyl alkyl/aryl thioethers and nitroso-substituted phenyl alkyl/aryl thioethers have been synthesized and tested for their mutagenicity towards Salmonella typhimurium strain TA100, TA98, TA98NR and TA98/1,8-DNP 6 in the absence of S9 mix. The relative order of mutagenicity in TA98 and TA100 among p-nitrophenyl thioethers having alkyl or aryl substituents is allyl > phenyl > benzyl > butyl > propyl > ethyl > methyl. Compounds having an alkyl chain C 6 to C 12 were found to be non-mutagenic. Among the various positional isomers (ortho, meta and para) of nitro-substituted diphenyl thioethers only the compounds having the-NO 2 function at the para position is mutagenic, whereas compounds having a-NO 2 function at ortho and meta are non-mutagenic. However, the reduced intermediate, ortho-nitroso derivative was found to be mutagenic in all the four strains but the meta-nitroso derivative was found to be non-mutagenic. All mutagens were found to be non-mutagenic when tested in nitroreductase deficient strain TA98NR, whereas their nitroso intermediates are found to be mutagenic. A substantial fall in the mutagenic activity is observed when some mutagens are tested in O-acetyltransferase deficient strain TA98/1,8-DNP 6 .
Ortho-, meta-and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and test... more Ortho-, meta-and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and tested for their mutagenicity toward Salmonella typhimurium TA100, TA100NR (nitroreductase deficient
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