[11C]Enzastaurin, the first design and radiosynthesis of a new potential PET agent for imaging of protein kinase C

Min Wang, Lu Xu, Mingzhang Gao, Kathy Miller, George W. Sledge, Qi-Huang Zheng

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

Enzastaurin (LY317615) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 value of ∼6 nM. [11C] Enzastaurin (3-(1-[11C]methyl-1H-indol-3-yl)-4-[1-[1-(2- pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of PKC, was first designed and synthesized in 20-25% 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
Pages (from-to)1649-1653
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number6
DOIs
StatePublished - Mar 15 2011

Fingerprint

Protein Kinase C
Maleic Anhydrides
Imaging techniques
Pyrroles
Protein C Inhibitor
Protein Kinase Inhibitors
Inhibitory Concentration 50
Carbon
enzastaurin
maleimide

Keywords

  • [C]Enzastaurin
  • Alzheimer's disease
  • Cancer
  • Positron emission tomography (PET)
  • Protein kinase C (PKC)
  • Radiosynthesis

ASJC Scopus subject areas

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

Cite this

[11C]Enzastaurin, the first design and radiosynthesis of a new potential PET agent for imaging of protein kinase C. / Wang, Min; Xu, Lu; Gao, Mingzhang; Miller, Kathy; Sledge, George W.; Zheng, Qi-Huang.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 6, 15.03.2011, p. 1649-1653.

Research output: Contribution to journalArticle

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AU - Sledge, George W.

AU - Zheng, Qi-Huang

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