1567375-93-2Relevant academic research and scientific papers
RADIOLABELED TRACERS FOR POLY (ADP-RIBOSE) POLYMERASE-1 (PARP-1), METHODS AND USES THEREFOR
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Page/Page column 10; 11; 12; 13, (2015/07/16)
Disclosed are PARP-1 inhibitors, which can be 18 F-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-triazatr
Synthesis, [18F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography
Zhou, Dong,Chu, Wenhua,Xu, Jinbin,Jones, Lynne A.,Peng, Xin,Li, Shihong,Chen, Delphine L.,Mach, Robert H.
, p. 1700 - 1707 (2014/03/21)
Imaging of poly (ADP-ribose) polymerase-1 (PARP-1) expression in vivo is a potentially powerful tool for developing PARP-1 inhibitors for drug discovery and patient care. We have synthesized several derivatives of benzimidazole carboxamide as PARP-1 inhibitors, which can be 18F-labeled easily for positron emission tomographic (PET) imaging. Of the compounds synthesized, 12 had the highest inhibition potency for PARP-1 (IC50 = 6.3 nM). [ 18F]12 was synthesized under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET studies using [ 18F]12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [18F]12 in the tumor that was blocked by olaparib, suggesting that the uptake of [18F]12 in the tumor is specific to PARP-1 expression.
