Nagao M, Wakabayashi K, Kasai H, Nishimura S, Sugimura T
Carcinogenesis. 1981;2(11):1147-9. doi: 10.1093/carcin/2.11.1147.
2-Amino-3-methylimidazo[4,5-f]quinoline [I] is a potent mutagen isolated from broiled sun-dried sardine. [I] and its seven of derivatives, (two isomers, one demethylated derivative and four methyl-substituted derivatives), were tested for mutagenicity on Salmonella typhimurium TA98 and TA100 in the presence of S9 mix. 2-Amino-1,4-dimethylimidazo[4,5-f]quinoline was the strongest mutagen of these 8 compounds on TA98, giving 159,000 revertants/nmol (750,000 revertants/micrograms). The demethylated derivative, 2-aminoimidazo[4,5-f]-quinoline, had very weak mutagenicity, inducing only 55 revertants/nmol (200 revertants/micrograms). Compounds having a methyl group at position N-1 or N-3 of 2-aminoimidazo[4,5]f]quinoline were strong mutagens. The 1,5-dimethy-derivative was more mutagenic than 3,5-dimethyl-derivative. Introduction of a methyl group at position 4 and position 5 enhanced and reduced the mutagenicity, respectively. All the compounds tested were more mutagenic to TA98 than to TA100, but their relative orders of mutgenicity with TA98 and TA100 were the same.
2-氨基-3-甲基咪唑并[4,5-f]喹啉[I]是从烤制的晒干沙丁鱼中分离出的一种强诱变剂。[I]及其七种衍生物（两种异构体、一种去甲基化衍生物和四种甲基取代衍生物）在存在S9混合物的情况下，针对鼠伤寒沙门氏菌TA98和TA100进行了诱变性测试。2-氨基-1,4-二甲基咪唑并[4,5-f]喹啉是这8种化合物中对TA98诱变作用最强的，产生159,000回复突变体/纳摩尔（750,000回复突变体/微克）。去甲基化衍生物2-氨基咪唑并[4,5-f]喹啉具有非常弱的诱变性，仅诱导55回复突变体/纳摩尔（200回复突变体/微克）。在2-氨基咪唑并[4,5]f]喹啉的N-1或N-3位具有甲基的化合物是强诱变剂。1,5-二甲基衍生物比3,5-二甲基衍生物的诱变性更强。在4位和5位引入甲基分别增强和降低了诱变性。所有测试的化合物对TA98的诱变性均比对TA100更强，但它们对TA98和TA100的诱变相对顺序相同。
