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Bioorg Med Chem Lett. 2013 Nov 1;23(21):5882-6. doi: 10.1016/j.bmcl.2013.08.087. Epub 2013 Sep 3.

2-Phenylbenzofuran derivatives alleviate mitochondrial damage via the inhibition of β-amyloid aggregation.

Author information

  • 1Integrated 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.

Abstract

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.

KEYWORDS:

2-Phenylbenzofuran; Alzheimer’s disease; Aβ aggregation inhibitor; Mitochondria

PMID:
24076170
DOI:
10.1016/j.bmcl.2013.08.087
[PubMed - indexed for MEDLINE]
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