Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:16

Article

Lafite, P ; Dijols, S ; Buisson, D ; Macherey, AC ; Zeldin, DC ; Dansette, PM ; Mansuy, D

关键词: cardiovascular system;    terfenadine;    ebastine;    hydroxylation;    suicide substrates;    monooxygenases;   

DOI  :  10.1016/j.bmcl.2006.02.004

来源: Elsevier

【 摘 要 】

The active site topology, substrate specificity, and biological roles of the human cytochrome P450 CYP2J2, which is mainly expressed in the cardiovascular system, are poorly known even though recent data suggest that it Could be a novel biomarker and potential target for therapy of human cancer. This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with K-i values as low as 160 nM, that should be useful tools to determine the biological roles of CYP2J2. (C) 2006 Elsevier Ltd. All rights reserved.

【 授权许可】

Free