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Evaluation of the Antiprion Activity of 6-aminophenanthridines and Related Heterocycles

Evaluation of the Antiprion Activity of 6-aminophenanthridines and Related Heterocycles

Phuhai Nguyen, Nassima Oumata, Flavie Soubigou, Justine Evrard, Nathalie Desban, Pascale Lemoine, Serge Bouaziz, Marc Blondel, Cécile Voisset

Eur J Med Chem. 2014 Jul 23;82:363-71.

PMID: 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP832688	6-Aminophenanthridine		832-68-8	Price

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