Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein-protein interactions in prions

被引：18
作者：
Tran, Hoang Ngoc Ai [2 ]
Bongarzone, Salvatore [3 ,4 ]
Carloni, Paolo [3 ,4 ]
Legname, Giuseppe [2 ,4 ]
Bolognesi, Maria Laura [1 ]
机构：
[1] Alma Mater Studiorum Bologna Univ, Dept Pharmaceut Sci, I-40126 Bologna, Italy
[2] SISSA, Int Sch Adv Studies, Neurobiol Sector, I-34151 Trieste, Italy
[3] SISSA, Int Sch Adv Studies, Stat & Biol Phys Sector, I-34151 Trieste, Italy
[4] Italian Inst Technol, SISSA Unit, I-34151 Trieste, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 06期
关键词：
Prion diseases; Conformational diseases; Library design and synthesis; NEURODEGENERATIVE DISEASES; INTERACTION INHIBITORS; ALZHEIMERS-DISEASE; THERAPEUTIC AGENTS; AGGREGATION; MECHANISM; PEPTIDES; PROGRESS;
D O I：
10.1016/j.bmcl.2010.01.149
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：1866 / 1868
页数：3
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