Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to β-amyloid fibrils

Hyu Ji Lee, Soo Jeong Lim, Seung Jun Oh, Dae Hyuk Moon, Dong Jin Kim, Jinsung Tae, Kyung Ho Yoo

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)


Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones 1a-k and isoindol-1-ones 2a-l were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated Aβ42 fibrils using [125I]TZDM. All the isoindolone derivatives showed very good binding affinities with Ki values in the subnanomolar range (0.42-0.94 nM). Among them, isoindol-1,3-diones 1i and 1k and isoindol-1-ones 2c and 2i exhibited excellent binding affinities (Ki = 0.42-0.44 and 0.46-0.49 nM) than those of Indoprofen (Ki = 0.52 nM) and PIB (Ki = 0.70 nM). These results suggest that isoindolones could be served as a scaffold for potential AD diagnostic probes to monitor Aβ fibrils.

Original languageEnglish
Pages (from-to)1628-1631
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 2008 Mar 1

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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