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000201266 1001_ $$0P:(DE-HGF)0$$aBongarzone, Salvatore$$b0
000201266 245__ $$aParallel Synthesis, Evaluation, and Preliminary Structure−Activity Relationship of 2,5-Diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound
000201266 260__ $$aWashington, DC$$bACS$$c2010
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000201266 520__ $$aA library of 11 entries, featuring a 2,5-diamino-1,4-benzoquinones nucleus as spacer connecting two aromatic prion recognition motifs, was designed and evaluated against prion infection. Notably, 6-chloro-1,2,3,4-tetrahydroacridine 10 showed an EC50 of 0.17 μM, which was lower than that displayed by reference compound BiCappa. More importantly, 10 possessed the capability to contrast prion fibril formation and oxidative stress, together with a low cytotoxicity. This study further corroborates the bivalent strategy as a viable approach to the rational design of anti-prion chemical probes.
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000201266 7001_ $$0P:(DE-HGF)0$$aTran, Hoang Ngoc Ai$$b1
000201266 7001_ $$0P:(DE-HGF)0$$aCavalli, Andrea$$b2
000201266 7001_ $$0P:(DE-HGF)0$$aRoberti, Marinella$$b3
000201266 7001_ $$0P:(DE-Juel1)145614$$aCarloni, Paolo$$b4$$ufzj
000201266 7001_ $$0P:(DE-HGF)0$$aLegname, Giuseppe$$b5$$eCorresponding Author
000201266 7001_ $$0P:(DE-HGF)0$$aBolognesi, Maria Laura$$b6$$eCorresponding Author
000201266 773__ $$0PERI:(DE-600)1491411-6$$a10.1021/jm100882t$$gVol. 53, no. 22, p. 8197 - 8201$$n22$$p8197 - 8201$$tJournal of medicinal chemistry$$v53$$x1520-4804$$y2010
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