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).
Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein-protein interactions in prions
BOLOGNESI, MARIA LAURA
2010
Abstract
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).File in questo prodotto:
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