TY  - JOUR
AU  - Bongarzone, Salvatore
AU  - Tran, Hoang Ngoc Ai
AU  - Cavalli, Andrea
AU  - Roberti, Marinella
AU  - Carloni, Paolo
AU  - Legname, Giuseppe
AU  - Bolognesi, Maria Laura
TI  - Parallel Synthesis, Evaluation, and Preliminary Structure−Activity Relationship of 2,5-Diamino-1,4-benzoquinones as a Novel Class of Bivalent Anti-Prion Compound
JO  - Journal of medicinal chemistry
VL  - 53
IS  - 22
SN  - 1520-4804
CY  - Washington, DC
PB  - ACS
M1  - FZJ-2015-03571
SP  - 8197 - 8201
PY  - 2010
AB  - 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.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000284287200029
DO  - DOI:10.1021/jm100882t
UR  - https://juser.fz-juelich.de/record/201266
ER  -