Nesnow S
J Med Chem. 1979 Oct;22(10):1244-7. doi: 10.1021/jm00196a018.
A series of substituted and structural analogues of 7,8-benzoflavone 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 which were found to be 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 which is either unsubstituted or substituted with an oxidizable moiety.
研究了一系列7,8-苯并黄酮的取代类似物和结构类似物，考察它们抑制由3-甲基胆蒽和苯巴比妥诱导的大鼠制备的肝微粒体中混合功能氧化酶对苯并[a]芘氧化的能力。在所有测试的苯并黄酮中，只有6-氨基-7,8-苯并黄酮对这两类诱导型混合功能氧化酶具有显著的抑制活性。发现最大抑制活性所需的参数包括：在2位保持未取代或特定取代的环外苯基、保留吡喃-4-酮环以及6位未取代或被可氧化部分取代。
