Synthesis and Biological Evaluation of a Fluorine-18 Derivative of Dasatinib
Journal of Medicinal Chemistry2007Vol. 50(23), pp. 5853–5857
Citations Over TimeTop 20% of 2007 papers
Darren R. Veach, Mohammad Namavari, Nagavarakishore Pillarsetty, Elmer Santos, Tatiana Beresten-Kochetkov, C Lambek, Blesida Punzalan, Christophe Antczak, Peter Smith‐Jones, Hakim Djaballah, Bayard Clarkson, Steven M. Larson
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.
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