| 摘要 |
Disclosed arc PARP-1 inhibitors, which can be 18P-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1,3,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC50=6.3 nM). Synthesis of [18F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield, MicroPET imaging using [18F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [18F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging. |
