Literature DB >> 17956080

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

Darren R Veach1, 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.   

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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Year:  2007        PMID: 17956080     DOI: 10.1021/jm070342g

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  17 in total

Review 1.  Molecular imaging for personalized cancer care.

Authors:  Moritz F Kircher; Hedvig Hricak; Steven M Larson
Journal:  Mol Oncol       Date:  2012-03-10       Impact factor: 6.603

2.  Novel derivatives of anaplastic lymphoma kinase inhibitors: Synthesis, radiolabeling, and preliminary biological studies of fluoroethyl analogues of crizotinib, alectinib, and ceritinib.

Authors:  Bhasker Radaram; Federica Pisaneschi; Yi Rao; Ping Yang; David Piwnica-Worms; Mian M Alauddin
Journal:  Eur J Med Chem       Date:  2019-08-09       Impact factor: 6.514

3.  Controlling cellular distribution of drugs with permeability modifying moieties.

Authors:  Paul L Richardson; Violeta L Marin; Stormy L Koeniger; Aleksandra Baranczak; Julie L Wilsbacher; Peter J Kovar; Patricia E Bacon-Trusk; Min Cheng; Todd A Hopkins; Sandra T Haman; Anil Vasudevan
Journal:  Medchemcomm       Date:  2019-04-18       Impact factor: 3.597

4.  Development of inverse electron demand Diels-Alder ligation and TR-FRET assays for the determination of ligand-protein target occupancy in live cells.

Authors:  Jasmina Marjanovic; Aleksandra Baranczak; Violeta Marin; Henning Stockmann; Paul L Richardson; Anil Vasudevan
Journal:  Medchemcomm       Date:  2017-02-21       Impact factor: 3.597

5.  In vivo imaging of Bcr-Abl overexpressing tumors with a radiolabeled imatinib analog as an imaging surrogate for imatinib.

Authors:  Athanasios P Glekas; Nagavara Kishore Pillarsetty; Blesida Punzalan; Nahida Khan; Peter Smith-Jones; Steven M Larson
Journal:  J Nucl Med       Date:  2011-07-15       Impact factor: 10.057

6.  Cell treatment and lysis in 96-well filter-bottom plates for screening Bcr-Abl activity and inhibition in whole-cell extracts.

Authors:  Michael R Mand; Ding Wu; Darren R Veach; Stephen J Kron
Journal:  J Biomol Screen       Date:  2010-03-17

7.  Dosimetry of 18F-labeled tyrosine kinase inhibitor SKI-249380, a dasatinib-tracer for PET imaging.

Authors:  Mark P S Dunphy; Pat Zanzonico; Darren Veach; Romel Somwar; Nagavarakishore Pillarsetty; Jason Lewis; Steven Larson
Journal:  Mol Imaging Biol       Date:  2012-02       Impact factor: 3.488

8.  Synthesis of a [(18)F]-labeled ceritinib analogue for positron emission tomography of anaplastic lymphoma kinase, a receptor tyrosine kinase, in lung cancer.

Authors:  Sandun Perera; David Piwnica-Worms; Mian M Alauddin
Journal:  J Labelled Comp Radiopharm       Date:  2016-02-08       Impact factor: 1.921

9.  2-18F-Fluoropropionic acid as a PET imaging agent for prostate cancer.

Authors:  Nagavarakishore Pillarsetty; Blesida Punzalan; Steven M Larson
Journal:  J Nucl Med       Date:  2009-09-16       Impact factor: 10.057

10.  (124)I-iodopyridopyrimidinone for PET of Abl kinase-expressing tumors in vivo.

Authors:  Mikhail Doubrovin; Tatiana Kochetkova; Elmer Santos; Darren R Veach; Peter Smith-Jones; Nagavarakishore Pillarsetty; Julius Balatoni; William Bornmann; Juri Gelovani; Steven M Larson
Journal:  J Nucl Med       Date:  2010-01       Impact factor: 10.057

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