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

Hoang Ngoc Ai Tran; Salvatore Bongarzone; Paolo Carloni; Giuseppe Legname; Maria Laura Bolognesi

doi:10.1016/j.bmcl.2010.01.149

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

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1866-8. doi: 10.1016/j.bmcl.2010.01.149. Epub 2010 Feb 4.

Authors

Hoang Ngoc Ai Tran¹, Salvatore Bongarzone, Paolo Carloni, Giuseppe Legname, Maria Laura Bolognesi

Affiliation

¹ Neurobiology Sector, International School for Advanced Studies (SISSA), Trieste, Italy.

PMID: 20172720
DOI: 10.1016/j.bmcl.2010.01.149

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzoquinones / chemical synthesis*
Benzoquinones / chemistry
Cell Line
Molecular Probes*
Prions / chemistry*
Protein Binding
Proteins / chemistry*

Substances

Benzoquinones
Molecular Probes
Prions
Proteins