Evaluation of the antiprion activity of 6-aminophenanthridines and related heterocycles.
Eur J Med Chem
; 82: 363-71, 2014 Jul 23.
Article
en En
| MEDLINE
| ID: mdl-24927056
ABSTRACT
Series of 6-aminophenanthridines and related heterocyclic compounds such as benzonaphtyridines were prepared. Reduction of one of the three aromatic rings was also performed. The compounds were first tested for their antiprion activity in a previously described yeast-based colourimetric prion assay. The most potent derivatives were then assayed ex vivo against the mammalian prion PrP(Sc) in a cell-based assay. Several of the new compounds were found more potent than the parent lead 6-aminophenanthridine. The most promising compounds against yeast and mammalian prions were 8-azido-6-aminophenanthridine (3m), and 7,10-dihydrophenanthridin-6-amine (14). In the mammalian cell-based assay, the IC50 of these two compounds were around 5 µM and 1.8 µM, respectively.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fenantridinas
/
Priones
/
Compuestos Heterocíclicos
Límite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Año:
2014
Tipo del documento:
Article
País de afiliación:
Francia