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 IC(50) value of ∼6 nM. [(11)C]Enzastaurin (3-(1-[(11)C]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.
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
authors.forename: Min
authors.initials: M
authors.lastname: Wang
authors.forename: Lu
authors.initials: L
authors.lastname: Xu
authors.forename: Mingzhang
authors.initials: M
authors.lastname: Gao
authors.forename: Kathy D
authors.initials: KD
authors.lastname: Miller
authors.forename: George W
authors.initials: GW
authors.lastname: Sledge
authors.forename: Qi-Huang
authors.initials: QH
authors.lastname: Zheng
mesh_terms: D002247:Carbon Isotopes; D015195:Drug Design; D007211:Indoles / Q000737:chemistry*; D049268:Positron-Emission Tomography; D011493:Protein Kinase C / Q000378:metabolism*
chemical_list: D002247:Carbon Isotopes; D007211:Indoles; D011493:Protein Kinase C; C504878:enzastaurin