title: Radiosynthesis of [11C]Vandetanib and [11C]chloro-Vandetanib as new potential PET agents for imaging of VEGFR in cancer.
abstract: Vandetanib (ZD6474) and its chlorine analogue chloro-Vandetanib are potent and selective vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors with low nanomolar IC(50) values. [(11)C]Vandetanib and [(11)C]chloro-Vandetanib, new potential PET agents for imaging of VEGFR in cancer, were first designed, synthesized and labeled at nitrogen and oxygen positions from their corresponding N- and O-des-methylated precursors, in 40-50% decay corrected radiochemical yield and 370-555GBq/μmol specific activity at end of bombardment (EOB).
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
authors.forename: Mingzhang
authors.initials: M
authors.lastname: Gao
authors.forename: Christian M
authors.initials: CM
authors.lastname: Lola
authors.forename: Min
authors.initials: M
authors.lastname: Wang
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: D002250:Carbon Radioisotopes; D002713:Chlorine / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008745:Methylation; D015394:Molecular Structure; D009369:Neoplasms / Q000175:diagnosis* / Q000188:drug therapy; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D049268:Positron-Emission Tomography; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors / Q000737:chemistry*
chemical_list: D002250:Carbon Radioisotopes; D010880:Piperidines; D011799:Quinazolines; D019275:Radiopharmaceuticals; D002713:Chlorine; D040262:Receptors, Vascular Endothelial Growth Factor; C452423:vandetanib