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

Darren R. Veach, 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

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

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.

Original languageEnglish
Pages (from-to)5853-5857
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number23
DOIs
StatePublished - 15 Nov 2007
Externally publishedYes

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