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 [(11)C]CH3OTf through O-[(11)C]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[(18)F]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.
authors: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Indianapolis, IN 46202, USA.
authors: Mingzhang
authors: M
authors: Gao
authors: Qingqing
authors: Q
authors: Yang
authors: Min
authors: M
authors: Wang
authors: Kathy D
authors: KD
authors: Miller
authors: George W
authors: GW
authors: Sledge
authors: Qi-Huang
authors: QH
authors: Zheng
mesh_terms: D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry; D002250:Carbon Radioisotopes / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000201:enzymology; D009422:Nervous System Diseases / Q000000981:diagnostic imaging / Q000201:enzymology; D055601:Organic Chemistry Phenomena; D049268:Positron-Emission Tomography / Q000379:methods*; D019704:Protein Disulfide-Isomerases / Q000037:antagonists & inhibitors*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D002243:Carbolines; D002250:Carbon Radioisotopes; D004791:Enzyme Inhibitors; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D019704:Protein Disulfide-Isomerases