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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Veach DR,Namavari M,Pillarsetty N,Santos EB,Beresten-Kochetkov T,Lambek C,Punzalan BJ,Antczak C,Smith-Jones PM,Djaballah H,Clarkson B,Larson SM

doi

10.1021/jm070342g

subject

Has Abstract

pub_date

2007-11-15 00:00:00

pages

5853-7

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

50

pub_type

杂志文章

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