In 2014, Denora et al. published a report on anew selective bifunctionalchelating ligand of TSPO with potential activity against glioma celllines.69 The structural template of a previouslyreported 87 was used to design ligand 88, and a multi-step synthetic protocol was employed for the synthesis.The results of the biological evaluation revealed that 88 was endowed with an excellent affinity toward TSPO with Ki = 239 nM. Here, TSPO is linked to central nervous system cancer.