Parallel Synthesis, Evaluation, and Preliminary Structure−Activity Relationship of 2,5-Diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound
Parallel Synthesis, Evaluation, and Preliminary Structure−Activity Relationship of 2,5-Diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound
A 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...
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Personal Name(s): | Bongarzone, Salvatore |
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Tran, Hoang Ngoc Ai / Cavalli, Andrea / Roberti, Marinella / Carloni, Paolo / Legname, Giuseppe (Corresponding Author) / Bolognesi, Maria Laura (Corresponding Author) | |
Contributing Institute: |
Computational Biomedicine; IAS-5 GRS; GRS |
Published in: | Journal of medicinal chemistry, 53 (2010) 22, S. 8197 - 8201 |
Imprint: |
Washington, DC
ACS
2010
|
DOI: |
10.1021/jm100882t |
Document Type: |
Journal Article |
Research Program: |
ohne Topic |
Publikationsportal JuSER |
A 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. |