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卤代烃的化学结构、反应活性及致癌性。

Chemical structure, reactivity, and carcinogenicity of halohydrocarbons.

作者信息

Van Duuren B L

出版信息

Environ Health Perspect. 1977 Dec;21:17-23. doi: 10.1289/ehp.772117.

Abstract

This review summarizes studies concerning the covalent binding of [14C]TCE to rat liver microsomal protein and exogenous DNA, in vitro, the enhancement of this binding by inducers of mixed-function oxidases, and inhibition of binding by inhibitors of these enzymes. Furthermore, recent studies on this type of binding in various strains of mice and rats of both sexes and using microsomal preparations from various organs are briefly reviewed. Other work reviewed here concerns the synthesis of TCE epoxide and its reaction with nucleophiles since it is believed that TCE epoxide is the activated carcinogenic intermediate of TCE. The utility of structural prognostication of carcinogenic activity and the importance of considering possible metabolic pathways for other chlorinated olefins is also discussed.

摘要

本综述总结了有关[14C]三氯乙烯(TCE)与大鼠肝脏微粒体蛋白及外源性DNA共价结合的研究,包括体外实验中混合功能氧化酶诱导剂对这种结合的增强作用,以及这些酶的抑制剂对结合的抑制作用。此外,还简要回顾了近期在不同品系的雌雄小鼠和大鼠中,使用来自不同器官的微粒体制剂进行的此类结合研究。这里回顾的其他工作涉及TCE环氧化物的合成及其与亲核试剂的反应,因为人们认为TCE环氧化物是TCE的活性致癌中间体。还讨论了致癌活性结构预测的实用性以及考虑其他氯化烯烃可能代谢途径的重要性。

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Carcinogenic activity of alkylating agents.烷化剂的致癌活性。
J Natl Cancer Inst. 1974 Sep;53(3):695-700. doi: 10.1093/jnci/53.3.695.

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