Kim, Kyoungdo Park, Kwang-su Kim, Mi Kyoung Choo, Hyunah Chong, Youhoon 2024-01-20T06:02:27Z 2024-01-20T06:02:27Z 2021-09-05 2015-10 1477-0520 https://pubs.kist.re.kr/handle/201004/124943 A series of novel J147 derivatives were synthesized, and their inhibitory activities against beta-amyloid (A beta) aggregation and toxicity were evaluated by using the oligomer-specific antibody assay, the thioflavin-T fluorescence assay, and a cell viability assay in the transformed SH-SY5Y cell culture. Among the synthesized J147 derivatives, 3j with a 2,2-dicyanovinyl substituent showed the most potent inhibitory activity against A beta(42) oligomerization (IC50 = 17.3 mu M) and A beta(42) fibrillization (IC50 = 10.5 mu M), and disassembled the preformed A beta(42) fibrils with an EC50 of 10.2 mu M. Finally, we confirmed that 3j is also effective at preventing neurotoxicity induced by A beta(42)-oligomers as well as A beta(42)-fibrils. English ROYAL SOC CHEMISTRY ALZHEIMERS-DISEASE COMMON MECHANISM SMALL-MOLECULE AGGREGATION CURCUMIN NEUROTOXICITY POLYPEPTIDE TOXICITY FIBRILS IMPLIES Dicyanovinyl-substituted J147 analogue inhibits oligomerization and fibrillation of beta-amyloid peptides and protects neuronal cells from beta-amyloid-induced cytotoxicity Article 10.1039/c5ob01463h 1 ORGANIC & BIOMOLECULAR CHEMISTRY, v.13, no.37, pp.9564 - 9569 ORGANIC & BIOMOLECULAR CHEMISTRY 13 37 9564 9569 scie scopus 000361548700004 2-s2.0-84941905929 Chemistry, Organic Chemistry Article ALZHEIMERS-DISEASE COMMON MECHANISM SMALL-MOLECULE AGGREGATION CURCUMIN NEUROTOXICITY POLYPEPTIDE TOXICITY FIBRILS IMPLIES Alzheimer’s disease neurodegenerative disease β-amyloid aggregation toxicity