A preliminary structure-activity study of the mixed-function oxidase inhibitor, 7,8-benzoflavone

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Abstract
A series of substituted and structural analogs of 7,8-benzoflavone [7,8-BF] were examined for their ability to inhibit benzo[a]pyrene oxidation by the mixed-function oxidases found in hepatic microsomes prepared from 3-methylcholanthrene- and phenobarbital-induced rats. Of all the benzoflavones tested, only 6-amino-7,8-benzoflavone possessed significant inhibitory activity toward both classes of induced mixed-function oxidases. Parameters necessary for maximal inhibitory activity were the maintenance of an unsubstituted or specifically substituted exocyclic phenyl group on position 2, the preservation of the pyran-4-one ring and a 6 position either unsubstituted or substituted with an oxidizable moiety. [7,8-BF is used in mechanistic studies of the metabolic activation of carcinogens.].

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