Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer

Mingzhang Gao, Qingqing Yang, Min Wang, Kathy D. Miller, George W. Sledge, Qi Huang Zheng

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Carbon-11-labeled substituted Β-tetrahydrocarbolines were prepared from their corresponding phenolic hydroxyl precursors with [11C]CH3OTf through O-[11C]methylation and isolated by simplified SPE in 50-60& decay corrected radiochemical yields at EOB with 185-370GBq/μmol specific activity at EOS. A fluorine-18-labeled substituted Β-tetrahydrocarboline was prepared from its corresponding halo-precursors (X=Cl, Br, I) with K[18F]F/Kryptofix 2.2.2 via the nucleophilic substitution and isolated by HPLC combined with SPE in 25-40& decay corrected radiochemical yield with 37-222GBq/μmol specific activity at EOB.

Original languageEnglish (US)
Pages (from-to)61-69
Number of pages9
JournalApplied Radiation and Isotopes
Volume74
DOIs
StatePublished - Apr 1 2013

Keywords

  • Cancer
  • Neurological disorders
  • Positron emission tomography (PET)
  • Protein disulfide isomerase (PDI)
  • Radiolabeled substituted Β-tetrahydrocarbolines
  • Radiosynthesis

ASJC Scopus subject areas

  • Radiation

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