A comparison of mutagenic and carcinogenic activities of aniline mustards.
A set of 15 derivatives of aniline mustard (I) was tested to give a quantitative measure of mutagenicity in Salmonella typhimurium TA-1535 and TA-100 and also carcinogenicity as lung tumors in strain-A mice. The structural variation in the set was chosen to minimize collinearity between hydrophobic, electronic, and molar refractive properties. By these measures, there was not a direct relationship between mutagenicity and carcinogenicity; in fact, since the 4-OPh analogue ranked highest in mutagenicity and among the lowest in carcinogenicity, while the reverse was noted for the 3,5-(NHCONH2)2 analogue, an inverse relationship was marginally significant. S-9 activation was required in the Ames test using TA-100, and the dose-response curve, prior to toxicity, appeared biphasic.
D000236:Adenoma / Q000188:drug therapy; D000816:Aniline Mustard / Q000031:analogs & derivatives / Q000633:toxicity*; D000818:Animals; D002273:Carcinogens; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D009153:Mutagens; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009588:Nitrogen Mustard Compounds / Q000633:toxicity*
D002273:Carcinogens; D009153:Mutagens; D009588:Nitrogen Mustard Compounds; D000816:Aniline Mustard