Synthesis and biological evaluation of a novel decadentate ligand DEPA
Synthesis and biological evaluation of a novel decadentate ligand DEPA
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DOI：
10.1016/j.bmcl.2008.09.063
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发表时间：
2008-11-01
影响因子：
2.7
通讯作者：
Lewis, Michael R.
中科院分区：
文献类型：
--
作者：
Chong, Hyun-Soon;Lim, Sooyoun;Lewis, Michael R.
报道了一种具有大环和无环结合基团的新型十烯酸配体7-[2-（双羧甲基-氨基）-乙基]-4,10-双羧甲基-1,4,7,10-四氮杂环十二-1-基乙酸（DEPA）的高效、短合成路线。研究了DEPA前体分子1,4,7-三（叔丁基羰基甲基）四氮杂环十二烷的合成方法。DEPA作为（177）Lu, (212)Bi和（213）Bi的螯合剂，在基于偶氮胂III的光谱络合动力学、体外血清稳定性和体内生物分布研究的抗体靶向癌症治疗、放射免疫治疗（RIT）中具有潜在的应用前景。(C) 2008年Elsevier Ltd.出版
An efficient and short synthetic route to a novel decadentate ligand 7-[2-(bis-carboxymethyl-amino)-ethyl]-4,10-bis-carboxymethyl-1,4,7,10-tetraaza-cyclododec-1-yl-acetic acid (DEPA) with both macrocyclic and acyclic binding moieties is reported. A reproducible and scalable synthetic method to a precursor molecule of DEPA, 1,4,7-tris(tert-butoxycarbonylmethyl) tetraazacyclododecane was developed. DEPA was evaluated as a chelator of (177)Lu, (212)Bi, and (213)Bi for potential use in an antibody-targeted cancer therapy, radioimmunotherapy (RIT) using Arsenazo III based spectroscopic complexation kinetics, in vitro serum stability, and in vivo biodistribution studies. (C) 2008 Published by Elsevier Ltd.