Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein–protein interactions in prions

Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein–protein interactions in prions

A small library combining two different benzoquinone cores with seven ( l) amino acid methyl esters (alanine, Nω-nitro-arginine, Nε-BOC-lysine, isoleucine, methionine, phenylalanine and tryptophan) was prepared and tested for prion replication inhibition in ScGT1 cells. The most potent hit, 6a, disp...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1866-1868
Hauptverfasser: Tran, Hoang Ngoc Ai, Bongarzone, Salvatore, Carloni, Paolo, Legname, Giuseppe, Bolognesi, Maria Laura
Format: Artikel
Sprache:eng
Schlagworte:
Benzoquinones - chemical synthesis
Benzoquinones - chemistry
Biological and medical sciences
Cell Line
Conformational diseases
Library design and synthesis
Medical sciences
Miscellaneous
Molecular Probes
Neuropharmacology
Pharmacology. Drug treatments
Prion diseases
Prions - chemistry
Protein Binding
Proteins - chemistry
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Zusammenfassung:A small library combining two different benzoquinone cores with seven ( l) amino acid methyl esters (alanine, Nω-nitro-arginine, Nε-BOC-lysine, isoleucine, methionine, phenylalanine and tryptophan) was prepared and tested for prion replication inhibition in ScGT1 cells. The most potent hit, 6a, displayed an EC 50 value of 0.87 μM, which is very close to that of quinacrine (0.4 μM).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.149