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, Nomega-nitro-arginine, Nepsilon-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 microM, which is very close to that of quinacrine (0.4 microM).
Tran
Hoang Ngoc Ai
HN
Neurobiology Sector, International School for Advanced Studies (SISSA), Trieste, Italy.
Bongarzone
Salvatore
S
Carloni
Paolo
P
Legname
Giuseppe
G
Bolognesi
Maria Laura
ML
D016227:Benzoquinones / Q000138:chemical synthesis* / Q000737:chemistry; D002460:Cell Line; D015335:Molecular Probes; D011328:Prions / Q000737:chemistry*; D011485:Protein Binding; D011506:Proteins / Q000737:chemistry*
D016227:Benzoquinones; D015335:Molecular Probes; D011328:Prions; D011506:Proteins