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).
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
-
Carbon Radioisotopes
-
Chlorine* / chemistry
-
Humans
-
Inhibitory Concentration 50
-
Magnetic Resonance Spectroscopy
-
Methylation
-
Molecular Structure
-
Neoplasms / diagnosis*
-
Neoplasms / drug therapy
-
Piperidines / chemical synthesis
-
Piperidines / chemistry
-
Piperidines / pharmacology*
-
Piperidines / therapeutic use
-
Positron-Emission Tomography*
-
Quinazolines / chemical synthesis
-
Quinazolines / chemistry
-
Quinazolines / pharmacology*
-
Quinazolines / therapeutic use
-
Radiopharmaceuticals / chemical synthesis*
-
Radiopharmaceuticals / chemistry
-
Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors
-
Receptors, Vascular Endothelial Growth Factor / chemistry*
Substances
-
Carbon Radioisotopes
-
Piperidines
-
Quinazolines
-
Radiopharmaceuticals
-
Chlorine
-
Receptors, Vascular Endothelial Growth Factor
-
vandetanib