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

doi:10.1021/jm070342g

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 journal › Article › peer-review

40 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/p210^bcr-abl human leukemic cell growth. Using positron emission tomography, we visualized K562 tumor xenografts in mice with [¹⁸F]-5.

Original language	English
Pages (from-to)	5853-5857
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	50
Issue number	23
DOIs	https://doi.org/10.1021/jm070342g
State	Published - 15 Nov 2007
Externally published	Yes

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title = "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.",

author = "Veach, \{Darren R.\} and Mohammad Namavari and Nagavarakishore Pillarsetty and Santos, \{Elmer B.\} and Tatiana Beresten-Kochetkov and Caryl Lambek and Punzalan, \{Blesida J.\} and Christophe Antczak and Smith-Jones, \{Peter M.\} and Hakim Djaballah and Bayard Clarkson and Larson, \{Steven M.\}",

year = "2007",

month = nov,

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doi = "10.1021/jm070342g",

language = "English",

volume = "50",

pages = "5853--5857",

journal = "Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib

AU - Veach, Darren R.

AU - Namavari, Mohammad

AU - Pillarsetty, Nagavarakishore

AU - Santos, Elmer B.

AU - Beresten-Kochetkov, Tatiana

AU - Lambek, Caryl

AU - Punzalan, Blesida J.

AU - Antczak, Christophe

AU - Smith-Jones, Peter M.

AU - Djaballah, Hakim

AU - Clarkson, Bayard

AU - Larson, Steven M.

PY - 2007/11/15

Y1 - 2007/11/15

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/36148940956

U2 - 10.1021/jm070342g

DO - 10.1021/jm070342g

M3 - Article

C2 - 17956080

AN - SCOPUS:36148940956

SN - 0022-2623

VL - 50

SP - 5853

EP - 5857

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 23

ER -

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

Abstract

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