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

…, T Beresten-Kochetkov, C Lambek…

文献索引: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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被引用次数: 29

摘要

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 ...