Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib

  • J Med Chem. 2007 Nov 15;50(23):5853-7. doi: 10.1021/jm070342g.
Darren R Veach  1 ,  Mohammad Namavari ,  Nagavarakishore Pillarsetty ,  Elmer B Santos ,  Tatiana Beresten-Kochetkov ,  Caryl Lambek ,  Blesida J Punzalan ,  Christophe Antczak ,  Peter M Smith-Jones ,  Hakim Djaballah ,  Bayard Clarkson ,  Steven M Larson
Affiliations
  • 1. Department of Molecular Pharmacology and Chemistry, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA.
PMID: 17956080 DOI: 10.1021/jm070342g
Abstract

Tyrosine kinases often play pivotal roles in the pathogenesis of Cancer and are good candidates for therapeutic intervention and targeted molecular imaging. The precursor synthesis, radiosynthesis, and biological characterization of a fluorine-18 analog of dasatinib, a multitargeted kinase inhibitor, are reported. Compound 5 potently inhibits Abl, Src, and Kit kinases and inhibits K562 and M07e/p210bcr-abl human leukemic cell growth. Using positron emission tomography, we visualized K562 tumor xenografts in mice with [18F]-5.