Radiosynthesis of [11C]Vandetanib and [11C]chloro- Vandetanib as new potential PET agents for imaging of VEGFR in cancer

Mingzhang Gao, Christian M. Lola, Min Wang, Kathy Miller, George W. Sledge, Qi-Huang Zheng

Research output: Contribution to journalArticle

21 Citations (Scopus)

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 IC50 values. [ 11C]Vandetanib and [11C]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 370-555 GBq/μmol specific activity at end of bombardment (EOB).

Original languageEnglish
Pages (from-to)3222-3226
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number11
DOIs
StatePublished - Jun 1 2011

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Vascular Endothelial Growth Factor Receptor
Imaging techniques
Neoplasms
Chlorine
Protein-Tyrosine Kinases
Inhibitory Concentration 50
Nitrogen
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
Oxygen

Keywords

  • [C]Chloro-Vandetanib
  • [C]Vandetanib
  • Cancer
  • Positron emission tomography (PET)
  • Radiosynthesis
  • Vascular endothelial growth factor receptors (VEGFR)

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry
  • Medicine(all)

Cite this

Radiosynthesis of [11C]Vandetanib and [11C]chloro- Vandetanib as new potential PET agents for imaging of VEGFR in cancer. / Gao, Mingzhang; Lola, Christian M.; Wang, Min; Miller, Kathy; Sledge, George W.; Zheng, Qi-Huang.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 11, 01.06.2011, p. 3222-3226.

Research output: Contribution to journalArticle

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