Gallium-68 and scandium-44 labelled radiotracers based on curcumin structure linked to bifunctional chelators: Synthesis and characterization of potential PET radiotracers
作者:Giulia Orteca、Jean-Philippe Sinnes、Sara Rubagotti、Michele Iori、Pier Cesare Capponi、Markus Piel、Frank Rösch、Erika Ferrari、Mattia Asti
DOI:10.1016/j.jinorgbio.2019.110954
日期:2020.3
metal complexes showed widespread applications in medicine and can be exploited as a lead structure for developing new tracers for nuclear medicine application. Herein, the synthesis, chemical characterization and radiolabelling with gallium-68 and scandium-44 of two new targeting vectors based on curcumin scaffolds and linked to the chelators 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA)
姜黄素金属配合物在医学中显示出广泛的应用,并且可以被用作开发用于核医学应用的新示踪剂的先导结构。在本文中,基于姜黄素支架并与螯合剂1,4,7-三氮杂环壬烷,1-戊二酸-4,7-乙酸连接的两个新的靶向载体的镓68和scan44的合成,化学表征和放射性标记据报道(NODAGA)和1,4-双(羧甲基)-6- [双(羧甲基)]氨基-6-甲基过氢-1,4-二氮杂(AAZTA)。可以以13%和11%的产率实现前体的合成,并且放射性标记通常可在温和条件下(> 95%)迅速掺入。在生理介质中的稳定性([68Ga] Ga-/ [44Sc] Sc-AAZTA-PC21在人血中2小时后约为75%,[68Ga] Ga-NODAGA-C21为约60%,如果与先前放射性标记的类似物相比,则通常被增强。MSn碎片实验显示,主要是由于姜黄素酮-烯醇部分的吡唑衍生化,AAZTA-PC21结构具有很高的稳定性,而镓68和scan