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 Miller, George W. Sledge, Qi-Huang Zheng

Research output: Contribution to journalArticle

7 Citations (Scopus)

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

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disulfides
inhibitors
enzymes
cancer
disorders
proteins
methylation
decay
synthesis
fluorine
halos
substitutes
carbon

Keywords

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

ASJC Scopus subject areas

  • Radiation

Cite this

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title = "Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer",
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.",
keywords = "Cancer, Neurological disorders, Positron emission tomography (PET), Protein disulfide isomerase (PDI), Radiolabeled substituted Β-tetrahydrocarbolines, Radiosynthesis",
author = "Mingzhang Gao and Qingqing Yang and Min Wang and Kathy Miller and Sledge, {George W.} and Qi-Huang Zheng",
year = "2013",
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journal = "Applied Radiation and Isotopes",
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TY - JOUR

T1 - Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer

AU - Gao, Mingzhang

AU - Yang, Qingqing

AU - Wang, Min

AU - Miller, Kathy

AU - Sledge, George W.

AU - Zheng, Qi-Huang

PY - 2013/4

Y1 - 2013/4

N2 - 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.

AB - 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.

KW - Cancer

KW - Neurological disorders

KW - Positron emission tomography (PET)

KW - Protein disulfide isomerase (PDI)

KW - Radiolabeled substituted Β-tetrahydrocarbolines

KW - Radiosynthesis

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