Synthesis and evaluation of novel PD-L1-targeted small molecules for 18F-labeling and PET imaging

Conclusions: To develop small molecule-based PD-L1 PET imaging probes, we designed and synthesized a library of fluorinated PD-L1 ligands based on the biphenyl pharmacophore. In vitro binding assay showed that several of the compounds possess nano-molar affinities to human PD-L1, and are potential PD-L1 PET imaging probe candidates. The radiolabeling and in vitro and in vivo pharmacology and pharmacokinetics studies of these PET tracers are under the way. Figure 1. The structure of the lead compound and the regions for SAR

Source: Journal of Nuclear Medicine - May 20, 2019 Category: Nuclear Medicine Authors: Wu, X., Pracitto, R., Pan, L., Li, L., Cai, Z. Tags: Novel Radiochemistry for Cancer Applications Source Type: research