Convenient Synthesis and Evaluation of Heptadentate Bifunctional Ligand for Radioimmunotherapy Applications.
Convenient Synthesis and Evaluation of Heptadentate Bifunctional Ligand for Radioimmunotherapy Applications.
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DOI：
10.1002/ejoc.201101063
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发表时间：
2011-11-01
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;Dong, Pengfei;Kang, Chi Soo
关键词：
开发了一种用于抗体靶向放射免疫治疗（RIT）的双功能螯合剂C-NE3TA-NCS的高效合成途径。围绕双分子环化、氮化吡啶和氮化吡啶阳离子开环反应、还原胺化反应等关键反应步骤，探索了多种合成方法，以优化四氮基螯合物TANPA和C-NE3TA类似物的制备。将七齿C-NE3TA-NCS偶联到肿瘤靶向抗体上，并与六齿C-NOTA-NCS进行比较，研究其与镧系元素的放射标记反应动力学。与c - nota抗体偶联物相比，c - ne3ta抗体偶联物与90Y的络合动力学显著增强。本文报道的TANPA和C-NE3TA-NCS的合成方法在制备双官能团大环螯合剂方面具有广泛的应用前景。
An efficient synthetic route to a bifunctional chelating agent C-NE3TA-NCS for antibody-targeted radioimmunotherapy (RIT) applications was developed. Various synthetic methods centered on the key reaction steps including bimolecular cyclization, ring opening reactions of aziridine and aziridinium cations, and reductive aminiation were explored to optimize the preparation of a tetraaza-based chelate TANPA and C-NE3TA analogues. Heptadentate C-NE3TA-NCS was conjugated to a tumor targeting antibody and compared to hexadentate C-NOTA-NCS for radiolabeling reaction kinetics with lanthanides for RIT. C-NE3TA-antibody conjugate displayed significantly enhanced complexation kinetics with 90Y as compared to C-NOTA-antibody conjugate. The synthetic methods for TANPA and C-NE3TA-NCS reported herein have broad applications for preparation of bifunctioanl macrocyclic chelating agents.
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影响因子：
2.8
作者：
CLARKE, ET;MARTELL, AE
通讯作者：
MARTELL, AE
影响因子：
4.7
作者：
Chong, Hyun-Soon;Song, Hyun A.;Brechbiel, Martin W.
通讯作者：
Brechbiel, Martin W.
影响因子：
2.7
作者：
Chong, Hyun-Soon;Song, Hyun A.;Ma, Xiang
通讯作者：
Ma, Xiang
影响因子：
3.3
作者：
Vogler, H;Platzek, J;Press, WR
通讯作者：
Press, WR
影响因子：
50.5
作者：
Baselga, J
通讯作者：
Baselga, J