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4-Substituted 1-chloro-2-nitrobenzenes: structure-activity relationships and extension of the substrate model of rat glutathione S-transferase 4-4

EM van der Aar, MJ de Groot, T Bouwman…

文献索引:Van Der Aar, Ellen M.; De Groot, Marcel J.; Bouwman, Tialda; Bijloo, Greetje J.; Commandeur, Jan N. M.; Vermeulen, Nico P. E. Chemical Research in Toxicology, 1997 , vol. 10, # 4 p. 439 - 449

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被引用次数: 12

摘要

In the present study, eleven 4-substituted 1-chloro-2-nitrobenzenes were tested for their GSH conjugation capacity when catalyzed by base or rat glutathione S-transferase (GST) 4- 4. Kinetic parameters (ks and K m, k cat, and k cat/K m) were determined and subsequently used for the description of structure-activity relationships (SAR's). For this purpose, eight physicochemical parameters (electronic, steric, and lipophilic) of the substituents and five ...