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4-硝基吡啶1-氧化物衍生物的致癌性和致突变性

Carcinogenicity and mutagenicity of 4-nitropyridine 1-oxide derivatives.

作者信息

Takahashi K, Huang G F, Araki M, Kawazoe Y

出版信息

Gan. 1979 Dec;70(6):799-806.

PMID:395009
Abstract

Carcinogenicity and mutagenicity of 4-nitropyridine 1-oxide (4-NPO) and 7 kinds of its alkyl derivatives were tested on mice and on Salmonella typhimurium strains and Escherichia coli strains. 3-Methyl-4-NPO is the most potent carcinogen, followed by 3-ethyl-4-NPO and then 4-NPO. Mutagenicity was most potent in 3-methyl, 2,3-dimethyl, and 2,5-dimethyl derivatives, moderate in 4-NPO and 2-methyl and 2,6-dimethyl derivatives, and to a least extent in 3,5-dimethyl-4-NPO. Structure-mutagenicity relationship was discussed on the basis of molecular mechanism of the carcinogenesis of 4-nitroquinoline 1-oxide. Quantitative relationship between mutagenicity and carcinogenicity was not strictly found among the compounds examined.

摘要

对4-硝基吡啶1-氧化物(4-NPO)及其7种烷基衍生物进行了小鼠、鼠伤寒沙门氏菌菌株和大肠杆菌菌株的致癌性和致突变性测试。3-甲基-4-NPO是最有效的致癌物,其次是3-乙基-4-NPO,然后是4-NPO。致突变性在3-甲基、2,3-二甲基和2,5-二甲基衍生物中最强,在4-NPO、2-甲基和2,6-二甲基衍生物中中等,在3,5-二甲基-4-NPO中最弱。根据4-硝基喹啉1-氧化物致癌作用的分子机制讨论了结构-致突变性关系。在所检测的化合物中未严格发现致突变性与致癌性之间的定量关系。

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