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Title: Synthesis, 11C labeling and biological properties of derivatives of the tyrphostin AG957.
Austin Authors: Ackermann, Uwe ;Tochon-Danguy, Henri J ;Nerrie, Maureen;Nice, Edouard C;Sachinidis, John I;Scott, Andrew M 
Affiliation: Centre for PET, Austin Health, Heidelberg, VIC 3084, Australia
Issue Date: 1-May-2005
Publication information: Nuclear Medicine and Biology; 32(4): 323-8
Abstract: Four analogues of AG957, a known inhibitor of the tyrosine kinase p210(bcr-abl), have been synthesized and tested for their growth inhibitory effect against the BCR/ABL-positive FDrv210C cells as well as the epidermal growth factor (EGF) receptor-positive Baf/ERX cells. All compounds that can undergo oxidation to the corresponding quinone demonstrated inhibition of FDrv210C cells and Baf/ERX cells. Compounds that cannot become oxidized showed significantly less inhibition of BCR/ABL- or EGF receptor-mediated cell proliferation. The (11)C-labeled compounds were prepared by labeling 4-aminobenzoic acid using [(11)C]CH(3)I, which afforded the corresponding (11)C-labeled methyl ester in excellent yields. Subsequent condensation of the amino group with an appropriately substituted hydroxy benzaldehyde formed the respective Schiff base. Reduction of this compound with NaBH(3)CN gave the (11)C-labeled inhibitors in an overall radiochemical yield of 17.3+/-2.1% (n=3; not decay corrected) and an average specific radioactivity of 40 GBq/micromol (1.1 Ci/micromol) at the end of synthesis. The total synthesis time from EOB including HPLC purification and formulation was 45 min.
Gov't Doc #: 15878501
DOI: 10.1016/j.nucmedbio.2005.02.006
Journal: Nuclear medicine and biology
Type: Journal Article
Subjects: Carbon Radioisotopes.chemistry.diagnostic use.pharmacokinetics
Cell Line, Tumor
Cell Proliferation.drug effects
Isotope Labeling.methods
Leukemia, Myelogenous, Chronic, BCR-ABL Positive.metabolism.pathology.radionuclide imaging
Positron-Emission Tomography.methods
Radiopharmaceuticals.adverse effects.chemical synthesis.diagnostic use.pharmacokinetics
Tyrphostins.adverse effects.chemistry.diagnostic use.pharmacokinetics
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