Linked Life Data

15878501

Source:http://linkedlifedata.com/resource/pubmed/id/15878501

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2005-5-9
pubmed:abstractText
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.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0969-8051
pubmed:author
pubmed:issnType
Print
pubmed:volume
32
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
323-8
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
Synthesis, 11C labeling and biological properties of derivatives of the tyrphostin AG957.
pubmed:affiliation
Centre for PET, Austin Health, Heidelberg, VIC 3084, Australia. ackerman@petnm.unimelb.edu.au
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't, Evaluation Studies