Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 6, Pages 1866-1868Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.149
Keywords
Prion diseases; Conformational diseases; Library design and synthesis
Categories
Funding
- University of Bologna
- Friuli-Venezia-Giulia Region
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A small library combining two different benzoquinone cores with seven (L) amino acid methyl esters (alanine, N omega-nitro-arginine, N epsilon-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 EC50 value of 0.87 mu M, which is very close to that of quinacrine (0.4 mu M). (C) 2010 Elsevier Ltd. All rights reserved.
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