title: Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein-protein interactions in prions.
abstract: 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).
authors.affiliation: Neurobiology Sector, International School for Advanced Studies (SISSA), Trieste, Italy.
authors.forename: Hoang Ngoc Ai
authors.initials: HN
authors.lastname: Tran
authors.forename: Salvatore
authors.initials: S
authors.lastname: Bongarzone
authors.forename: Paolo
authors.initials: P
authors.lastname: Carloni
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Legname
authors.forename: Maria Laura
authors.initials: ML
authors.lastname: Bolognesi
mesh_terms: D016227:Benzoquinones / Q000138:chemical synthesis* / Q000737:chemistry; D002460:Cell Line; D015335:Molecular Probes; D011328:Prions / Q000737:chemistry*; D011485:Protein Binding; D011506:Proteins / Q000737:chemistry*
chemical_list: D016227:Benzoquinones; D015335:Molecular Probes; D011328:Prions; D011506:Proteins