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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).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tran HN,Bongarzone S,Carloni P,Legname G,Bolognesi ML

doi

10.1016/j.bmcl.2010.01.149

subject

Has Abstract

pub_date

2010-03-15 00:00:00

pages

1866-8

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00171-X

journal_volume

20

pub_type

杂志文章

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