Exploring the structure-activity relationship of benzylidene-2,3-dihydro-1H-inden-1-one compared to benzofuran-3(2H)-one derivatives as inhibitors of tau amyloid fibers

• Published in: European journal of medicinal chemistry Vol. 231; pp. 114139 - 114150
• Main Authors: Boukherrouba, Emeline, Larosa, Camille, Nguyen, Kim-Anh, Caburet, Jérémy, Lunven, Laurent, Bonnet, Hugues, Fortuné, Antoine, Boumendjel, Ahcène, Boucherle, Benjamin, Chierici, Sabine, Peuchmaur, Marine
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 05.03.2022; Elsevier
• Subjects: AcPHF6 peptide; Alzheimer Disease; Alzheimer's disease; Aurones; Benzofurans - chemistry; Benzofurans - pharmacology; Chemical Sciences; Chemistry, Medicinal; Humans; Indanones; Life Sciences; Life Sciences & Biomedicine; Medicinal Chemistry; Neurons and Cognition; Pharmacology & Pharmacy; Protein Aggregates; Science & Technology; Structure-Activity Relationship; Tau aggregation; tau Proteins - metabolism; AcPHF6 peptide; Indanones; Aurones; Alzheimer's disease; Tau aggregation; DESIGN; NATURALLY-OCCURRING AURONES; INDANONE DERIVATIVES; DISCOVERY; FILAMENTS; MUSHROOM; DISEASE; CHEMISTRY; AGGREGATION; SCAFFOLD; tau aggregation

Tauopathies, such as Alzheimer's disease, have been the subject of several hypotheses regarding the way to treat them. Hyperphosphorylation of tau protein leading to its aggregation is widely recognized as a key step in the development of these diseases resulting in neuronal dysfunction. The Ac...