作者: P. Nordeman , Z.P. Jayendra , E. Briard , S.C. Li , M. Larhed
DOI: 10.1016/J.EJPS.2020.105647
关键词: Leaving group 、 Ligand (biochemistry) 、 Radiochemistry 、 In vitro 、 Metabolism 、 Chemistry 、 Tosyl 、 Frozen section procedure 、 In vivo 、 Hsp90
摘要: Abstract Purpose With the ambition of improving management pancreatic neuroendocrine tumors (P-NETs), we developed and preliminary validated a novel fluorine-18 labelled HSP90 ligand. Methods A precursor containing methoxymethyl ethers protecting groups tosyl as leaving group was synthesized. The target compound labeled with nucleophilic 18F-fluoride subsequently removed hydrochloric acid before purification. In vitro cell- frozen section autoradiography in vivo animal studies were performed. Results successfully synthesized utilized 18F-radiolabeling giving 0.5-1.0 GBq pure product synthesis time 70 min. experiments indicated high specific binding, but showed no tumor uptake due to fast hepatobiliary metabolism excretion. Conclusions Despite unfavorable properties tracer, promising results from sections P-NETs surgical resection encourage us continue project aiming improvement tracer.