Metabolic N-hydroxylation. Use of substituent variation to modulate the in vitro bioactivation of 4-acetamidostilbenes

PE Hanna, RE Gammans, RD Sehon…

文献索引：Hanna, Patrick E.; Gammans, Richard E.; Sehon, Russell D.; Lee, Man-Kil Journal of Medicinal Chemistry, 1980 , vol. 23, # 9 p. 1038 - 1044

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被引用次数: 16

摘要

N-Hydroxylation is an obligate step in the bioactivation of carcinogenic aryl amides. Previous reports from this laboratory demonstrated that variation of the 4'substituent of trans- 4-acetamidostilbene (1) has a marked effect on the rate of its in vitro microsomal N- hydroxylation. In order to further investigate the effects of electronegative and aliphatic substituents, the 4'-CN, 4'-CH,, 4'-C (CH3),, and 4'-CF3 analogues of 1 were synthesized ...