Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib Journal Article
| Authors: | Veach, D. R.; Namavari, M.; Pillarsetty, N.; Santos, E. B.; Beresten-Kochetkov, T.; Lambek, C.; Punzalan, B. J.; Antczak, C.; Smith-Jones, P. M.; Djaballah, H.; Clarkson, B.; Larson, S. M. |
| Article 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. © 2007 American Chemical Society. |
| Keywords: | controlled study; unclassified drug; drug efficacy; nonhuman; drug targeting; positron emission tomography; radiopharmaceuticals; cell proliferation; mouse; animals; mice; proto-oncogene proteins c-kit; enzyme inhibition; image analysis; culture medium; animal experiment; animal model; cancer cell culture; drug potency; tumor xenograft; drug effect; enzyme activity; cell line, tumor; diagnostic imaging; dasatinib; drug synthesis; pyrimidines; carcinogenesis; mice, nude; evaluation; diagnostic value; positron-emission tomography; transplantation, heterologous; protein-tyrosine kinases; fluorine 18; src-family kinases; thiazoles; catalytic domain; reaction analysis; proton nuclear magnetic resonance; carbon nuclear magnetic resonance; fluorine radioisotopes; n (2 chloro 6 methylphenyl) 2 [6 [4 (2 fluoroethyl)piperazin 1 yl] 2 methylpyrimidin 4 ylamino]thiazole 5 carboxamide |
| Journal Title: | Journal of Medicinal Chemistry |
| Volume: | 50 |
| Issue: | 23 |
| ISSN: | 0022-2623 |
| Publisher: | American Chemical Society |
| Date Published: | 2007-11-15 |
| Start Page: | 5853 |
| End Page: | 5857 |
| Language: | English |
| DOI: | 10.1021/jm070342g |
| PUBMED: | 17956080 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 12" - "Export Date: 17 November 2011" - "CODEN: JMCMA" - "Source: Scopus" |
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