Cytochrome P450 2E1/2A6-Selective Inhibition by Halogenated Anilines on Metabolic Activation of Dimethylnitrosamine in Human Liver Microsomes

Phenotype Analysis of Human Cytochrome P450 2C9 Polymorphism Using a Panel of Fluorine-Substituted Benzo[h]quinolines as Inhibitors of Tolbutamide Hydroxylation

“…In fact, our previous study indicated that the inhibitory effects of the anilines on CYP2E1 were widely affected by the substituting fluorine's number and position. 8,9) In the present study, benzo[h]quinoline (BhQ) and its fluorinated derivatives, 3-F-, 5-F-, 6-F-, 9-F-, 10-F-, 3,6-diF-, 5,6-diF-, and 7,10-diF-BhQ (Fig. 1), were subjected to analysis of their inhibitory effects on the metabolism of tolbutamide by recombinant human CYP2C9.1, 2C9.2, and 2C9.3 to investigate the structure-inhibition selectivity relationships.…”