The first synthesis of [11C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3)

Min Wang, Mingzhang Gao, Kathy D. Miller, George W. Sledge, Gary D. Hutchins, Qi Huang Zheng

Research output: Contribution to journalArticle

26 Scopus citations

Abstract

SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM. [11C]SB- 216763 (3-(2,4-dichlorophenyl)-4-(1-[11C]methyl-1H-indol-3-yl)-1H- pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-555 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide.

Original languageEnglish (US)
Pages (from-to)245-249
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number1
DOIs
StatePublished - Jan 1 2011

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Keywords

  • [C]SB-216763
  • Alzheimer's disease
  • Cancer
  • Glycogen synthase kinase-3 (GSK-3)
  • Positron emission tomography (PET)
  • Radiosynthesis

ASJC Scopus subject areas

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

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