García E, Lopez-de-Cerain A, Gullón A, Arrarás J A, Monge A
Toxicología Genética, C.I.F.A., Universidad de Navarra, Pamplona, Spain.
Mutagenesis. 1992 Jan;7(1):31-5. doi: 10.1093/mutage/7.1.31.
The mutagenicity of ten triazinoindole derivatives was studied in bacteria. The compounds form part of a 3-(4'-substituted-benzylidenamino)-5H-1,2,3-triazin[5,4-b]in dol-4-one series and differ in the physicochemical properties of the substituent at the 4' position of the benzylidenamino group: -H, -OH, -COOH, -OCH3, -COOCH3, -NHCOCH3, -C1, -NO2, -C6H5, and -OC6H5. They were tested in the TA97, TA98, TA100, and TA102 strains of Salmonella typhimurium, both with and without metabolic activation, using the preincubation procedure. Only the derivatives with phenyl and phenoxy substituents were non-mutagenic. The remaining compounds significantly increased the number of His+ revertants and showed three patterns of activity based upon their mutagenic potency and their response to metabolic activation. Size and hydrophobicity of the 4'-substituents are the physicochemical characteristics that most differentiate the mutagenic triazinoindole derivatives from the nonmutagenic ones.
在细菌中研究了十种三嗪并吲哚衍生物的致突变性。这些化合物是3-(4'-取代苄叉氨基)-5H-1,2,3-三嗪并[5,4-b]吲哚-4-酮系列的一部分，苄叉氨基4'位取代基的物理化学性质不同：-H、-OH、-COOH、-OCH3、-COOCH3、-NHCOCH3、-Cl、-NO2、-C6H5和-OC6H5。使用预培养程序，在有和没有代谢激活的情况下，在鼠伤寒沙门氏菌的TA97、TA98、TA100和TA102菌株中对它们进行了测试。只有带有苯基和苯氧基取代基的衍生物无致突变性。其余化合物显著增加了His+回复突变体的数量，并根据其致突变能力和对代谢激活的反应表现出三种活性模式。4'-取代基的大小和疏水性是使致突变性三嗪并吲哚衍生物与非致突变性衍生物最有区别的物理化学特征。
