Title: [11C]Enzastaurin, the first design and radiosynthesis of a new potential PET agent for imaging of protein kinase C
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.
Publication Year: 2011
Publication Date: 2011-03-01
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 16
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