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

…, T Beresten-Kochetkov, C Lambek…

Index: Veach, Darren R.; Namavari, Mohammad; Pillarsetty, Nagavarakishore; Santos, Elmer B.; Beresten-Kochetkov, Tatiana; Lambek, Caryl; Punzalan, Blesida J.; Antczak, Christophe; Smith-Jones, Peter M.; Djaballah, Hakim; Clarkson, Bayard; Larson, Steven M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 23 p. 5853 - 5857

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Citation Number: 29

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 ...