2-Phenylbenzofuran derivatives alleviate mitochondrial damage via the inhibition of β-amyloid aggregation.
To obtain modulators for reducing mitochondrial damage by the inhibition of Aβ oligomer formation, 2-phenylbenzofuran derivatives were designed and prepared. Their inhibitory activity against Aβ fibril formation was screened using ThT fluorescence assay, and the effect of derivatives on mitochondrial function was evaluated using JC-1 and MTT assay. 2-Phenylbenzofuran derivatives with dimethylamino group at p-position had an excellent inhibitory activity against Aβ fibril formation. Particularly, compound 19m alleviated mitochondrial damage remarkably and possessed protective effects against Aβ-induced cytotoxicity.
Integrated Research Institute of Pharmaceutical Sciences, College of Pharmacy, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon, Gyeonggi-do 420-743, Republic of Korea.
Yun Suk
YS
Lee
Hye Yun
HY
Kim
Hea Mee
HM
Youn
Jae Hong
JH
Seo
YoungSoo
Y
Kim
Kye Jung
KJ
Shin
D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001562:Benzimidazoles / Q000494:pharmacology; D001572:Benzofurans / Q000737:chemistry* / Q000494:pharmacology*; D002232:Carbocyanines / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D051379:Mice; D008928:Mitochondria / Q000187:drug effects* / Q000473:pathology
D016229:Amyloid beta-Peptides; D001562:Benzimidazoles; D001572:Benzofurans; D002232:Carbocyanines; C068624:5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolocarbocyanine
2-Phenylbenzofuran; Alzheimer’s disease; Aβ aggregation inhibitor; Mitochondria