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1-苯基-3,3-二甲基三氮烯致癌作用过程中作为活性代谢产物的1-苯基-3-甲基三氮烯的化学结构与急性毒性之间的关系

Relation between the chemical structure and acute toxicity of 1-phenyl-3-methyltriazenes as activated metabolites during the carcinogenic action of 1-phenyl-3,3-dimethyltriazenes.

作者信息

Matrka M, Rambousek V, Zvĕrina V

出版信息

Neoplasma. 1978;25(2):153-6.

PMID:643120
Abstract

The mol LD50 values were correlated with Hammett sigma constants in terms of the Hansen empiric equation 6 for para substituted derivatives of 1-phenyl-3-methyltriazene. Good agreement was achieved and the line slope of the correlation, 0.3, is the same as that found during an identical experiment with derivatives of 1-phenyl-3,3-dimethyltriazene [1]. This is an indirect evidence that the considered mechanism of the interaction with biological substrate goes through the "activated carcinogen" - derivatives of 1-phenyl-3-methyltriazene, formed through the oxidative N-demethylation of the initial 1-phenyl-3,3-dimethyltriazenes.

摘要

根据汉森经验方程6,对于1-苯基-3-甲基三氮烯的对位取代衍生物,摩尔LD50值与哈米特σ常数相关。两者取得了良好的一致性,相关性的直线斜率为0.3,这与对1-苯基-3,3-二甲基三氮烯衍生物进行相同实验时得到的斜率相同[1]。这是一个间接证据,表明与生物底物相互作用的所考虑机制是通过“活化致癌物”——1-苯基-3-甲基三氮烯的衍生物进行的,该衍生物是由初始的1-苯基-3,3-二甲基三氮烯经氧化N-去甲基化形成的。

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