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

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.

Graphical abstractRadiosynthesis of [11C]Enzastaurin, a new potential PET agent for imaging of protein kinase C (PKC), is first reported.Figure optionsDownload full-size imageDownload as PowerPoint slide