Synthesis and Evaluation of an Enantiomerically Enriched Bifunctional Chelator for 64Cu-Based Positron Emission Tomography (PET) Imaging
Synthesis and Evaluation of an Enantiomerically Enriched Bifunctional Chelator for 64Cu-Based Positron Emission Tomography (PET) Imaging
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DOI：
10.1002/ejoc.201301499
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发表时间：
2014-02-01
影响因子：
2.8
通讯作者：
Kang, Chi Soo
中科院分区：
文献类型：
--
作者：
Chong, Hyun-Soon;Sun, Xiang;Kang, Chi Soo
本文报道了一种对映体富集的双功能螯合剂（S）-C-NE 3 TA的合成和评价。该双功能螯合剂通过氮丙啶离子的区域选择性和立体选择性开环而有效地制备。新的手性螯合剂在室温下立即且几乎完全结合到Cu-64上。相应的Cu-64-放射性标记的复合物在人血清中保持完整48小时，没有任何可测量的螯合转移，并耐受严格的EDTA挑战24小时。Cu-64-放射性标记的（S）-C-NE 3 TA复合物在小鼠中稳定，并产生良好的生物分布特征。体外和体内评价的结果表明，新的光学活性螯合剂是PET成像应用的一个有前途的候选者。
We report the synthesis and evaluation of an enantiomerically enriched bifunctional chelator, (S)-C-NE3TA. The bifunctional chelator was efficiently prepared by regioselective and stereoselective ring opening of an aziridinium ion. The new chiral chelator instantly and almost completely bound to Cu-64 at room temperature. The corresponding Cu-64-radiolabeled complex remained intact in human serum for 48 h without any measurable transchelation and was tolerant to a rigorous EDTA challenge for 24 h. The Cu-64-radiolabeled (S)-C-NE3TA complex was stable in mice and produced an excellent biodistribution profile. The results of the in vitro and in vivo evaluations indicate that the new optically active chelator is a promising candidate for PET imaging applications.