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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >The long and short of it:the influence of N-carboxyethyl versus N-carboxymethyl pendant arms on in vitro and in vivo behavior of copper complexes of cross-bridged tetraamine macrocycles
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The long and short of it:the influence of N-carboxyethyl versus N-carboxymethyl pendant arms on in vitro and in vivo behavior of copper complexes of cross-bridged tetraamine macrocycles

机译：它的长短：N-羧乙基和N-羧甲基侧链对交叉桥四胺大环铜配合物的体外和体内行为的影响

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摘要

A cross-bridged cyclam ligand bearing two N-carboxymethyl pendant arms(1)has been found to form a copper(n)complex that exhibits significantly improved biological behavior in recent research towards 64Cu-based radiopharmaceuticals.Both the kinetic inertness and resistance to reduction of Cu-1 are believed to be relevant to its enhanced performance.To explore the influence of pendant arm length on these properties,new cross-bridged cyclam and cyclen ligands with longer N-carboxyethyl pendant arms,2 and 4,and their respective copper(II)complexes have been synthesized.Both mono- as well as di-O-protonated forms of Cu-2 have also been isolated and structurally characterized.The spectral and structural properties of Cu-2 and Cu-4,their kinetic inertness in 5 M HC1,and electrochemical behavior have been obtained and compared to those of their N-carboxymethyl-armed homologs,Cu-1 and Cu-3.Only the cyclam-based Cu-1 and Cu-2 showed unusually high kinetic inertness towards acid decomplexation.While both of these complexes also exhibited quasi-reversible Cu(II)/Cu(I)reductions,Cu-2 is easier to reduce by a substantial margin of +400 mV,bringing it within the realm of physiological reductants.Similarly,of the cyclen-based complexes,Cu-4 is also easier to reduce than Cu-3 though both reductions are irreversible.Biodistribution studies of 64Cu-labeled 2 and 4 were performed in Sprague Dawley rats.Despite comparable acid inertness to their shorter-armed congeners,both longer-armed ligand complexes have poorer bio-clearance properties.This inferior in vivo behavior may be a consequence of their higher reduction potentials.
机译：在最近对64Cu基放射性药物的研究中，发现带有两个N-羧甲基侧链臂（1）的跨桥Cyclam配体形成了铜（n）络合物，该络合物表现出显着改善的生物学行为。动力学惰性和抗还原性认为Cu-1的铜离子与其增强性能有关。为了研究悬臂长度对这些性能的影响，研究了具有较长N-羧乙基悬臂2和4的新的交叉桥环素和环素配体，以及它们各自的铜合成了（II）配合物，还分离出了Cu-2的单-和双O质子化形式，并对其结构进行了表征.Cu-2和Cu-4的光谱和结构性质以及它们的动力学惰性获得了5 M HCl和电化学行为，并将其与N-羧甲基武装的同系物Cu-1和Cu-3进行了比较。只有基于Cyclam的Cu-1和Cu-2对酸具有极高的动力学惰性解复杂度尽管这两种配合物也都表现出准可逆的Cu（II）/ Cu（I）还原，但Cu-2较容易还原，其实质边际为+400 mV，使其在生理还原剂范围内。尽管这两种还原都是不可逆的，但基于Cyclon的复合物，Cu-4也比Cu-3更易于还原。在Sprague Dawley大鼠中进行了64Cu标记的2和4的生物分布研究。尽管酸惰性与其短臂同类物相当，两种长臂配体配合物均具有较差的生物清除性能，这种较差的体内行为可能是其还原电位较高的结果。

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