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

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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. doi: 10.1016/j.bmcl.2010.11.026.
Min Wang 1,  Mingzhang Gao,  Kathy D Miller,  George W Sledge,  Gary D Hutchins,  Qi-Huang Zheng
Affiliations

Affiliation

  • 1 Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
PMID: 21115250 DOI: 10.1016/j.bmcl.2010.11.026
Abstract

SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]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.

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