Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation

Ji Hun Byun; Hye Yun Kim; Young Soo Kim; Inhee Mook-Jung; Dong Jin Kim; Won Koo Lee; Kyung Ho Yoo

doi:10.1016/j.bmcl.2008.08.111

Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation

Ji Hun Byun, Hye Yun Kim, Young Soo Kim, Inhee Mook-Jung, Dong Jin Kim, Won Koo Lee, Kyung Ho Yoo

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

59 Citations (Scopus)

Abstract

The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC₅₀ = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC₅₀ = 0.80 μM) and IMSB (IC₅₀ = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.

Original language	English
Pages (from-to)	5591-5593
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.08.111
Publication status	Published - 2008 Oct 15

Bibliographical note

Funding Information:
We are grateful to the Ministry of Science and Technology (MOST) and Ministry of Commerce, Industry and Energy (MCIE) of Korea for financial support.

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2008.08.111

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title = "Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation",

abstract = "The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.",

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AU - Kim, Young Soo

AU - Mook-Jung, Inhee

AU - Kim, Dong Jin

AU - Lee, Won Koo

AU - Yoo, Kyung Ho

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Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation

Abstract

Bibliographical note

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