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filingDate 2015-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2019-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2019-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-106458935-B
titleOfInvention Radiolabeled tracers for poly(ADP-ribose) polymerase-1 (PARP-1), methods and uses thereof
abstract PARP-1 inhibitors are disclosed that can be labeled with 18 F for use as tracers for positron emission tomography (PET) imaging. Synthetic methods are also disclosed. In the synthesized compound, 2-[p-(2-fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]tridecane-2,4(13) , 5,7-tetraene-9-one (12) had the highest inhibitory potency against PARP-1 (IC 50 =6.3 nM). The synthesis of [ 18 F]-12 with high specific activity and 40-50% decay-corrected yield under conventional conditions is disclosed. [ 18 F]-12 accumulation in tumors was confirmed using micro-PET imaging of [ 18 F ]-12 in MDA-MB-436 tumor-bearing mice. Binding can be blocked by olaparib. The compound can be used for tumor imaging.
priorityDate 2014-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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