Synthesis and biological evaluation of coumarin derivatives as selective CYP2A6 inhibitors.
CYP2A6
CYP3A4
Coumarin
Structure–activity relationship
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 04 2023
15 04 2023
Historique:
received:
22
12
2022
revised:
16
02
2023
accepted:
24
02
2023
medline:
11
4
2023
pubmed:
9
3
2023
entrez:
8
3
2023
Statut:
ppublish
Résumé
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 IC
Identifiants
pubmed: 36889653
pii: S0960-894X(23)00084-7
doi: 10.1016/j.bmcl.2023.129206
pii:
doi:
Substances chimiques
Aryl Hydrocarbon Hydroxylases
EC 1.14.14.1
Cytochrome P-450 Enzyme Inhibitors
0
Cytochrome P-450 CYP3A
EC 1.14.14.1
Methoxsalen
U4VJ29L7BQ
Coumarins
0
Cytochrome P-450 CYP2A6
EC 1.14.14.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
129206Informations de copyright
Copyright © 2023 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.