Synthesis and biological evaluation of coumarin derivatives as selective CYP2A6 inhibitors.
Bioorg Med Chem Lett
; 86: 129206, 2023 04 15.
Article
em En
| MEDLINE
| ID: mdl-36889653
ABSTRACT
Cytochrome P450 2A6 (CYP2A6) inhibitors are expected to be suitable as smoking cessation aids and for cancer prevention. Because the typical coumarin-based CYP2A6 inhibitor methoxsalen also inhibits CYP3A4, unintended drug-drug interactions are still a concern. Therefore, the development of selective CYP2A6 inhibitors is desirable. In this study, we synthesized coumarin-based molecules, determined the IC50 values for CYP2A6 inhibition, verified the possibility of mechanism-based inhibition, and compared the selectivity for CYP2A6 versus CYP3A4. The results demonstrated that we developed CYP2A6 inhibitors that were more potent and selective than methoxsalen.
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Base de dados:
MEDLINE
Assunto principal:
Hidrocarboneto de Aril Hidroxilases
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article