Design, Synthesis, and Evaluation of [18F]BIBD-300 as a Positron Emission Tomography Tracer for Poly(ADP-Ribose) Polymerase-1
Wei Zheng,
Yong Huang,
Yi Xie
et al.
Abstract:Compounds 8a−j were designed to adjust the mode of interaction and lipophilicity of FTT by scaffold hopping and changing the length of the alkoxy groups. Compounds 8a, 8d, 8g, and BIBD-300 were screened for highaffinity PARP-1 through enzyme inhibition assays and are worthy of further evaluation. PET imaging of MCF-7 subcutaneous tumors with moderate expression of PARP-1 showed that compared to [ 18 F]FTT, [ 18 F]8a, [ 18 F]8d, and [ 18 F]8g exhibited greater nonspecific uptake, a lower target-to-nontarget rat… Show more
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