Journal article

Synthesis, C-11 labeling and biological properties of derivatives of the tyrphostin AG957

U Ackermann, HJ Tochon-Danguy, M Nerrie, EC Nice, JI Sachinidis, AM Scott

Nuclear Medicine and Biology | ELSEVIER SCIENCE INC | Published : 2005


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 excellen..

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University of Melbourne Researchers