Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones.
Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones.
复制标题
同二聚和异二聚双（氨基硫醇）氧合金属与铼（V）和锝（V）的配合物。
DOI：
10.1021/jm00033a010
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发表时间：
1994
影响因子：
7.3
通讯作者：
Katzenellenbogen,JA
中科院分区：
文献类型：
--
作者：
Chi,DY;O'Neil,JP;Anderson,CJ;Welch,MJ;Katzenellenbogen,JA
我们研究了制备形状类似于类固醇受体配体的锝和锝配合物的可能性。氧化铼（V）和氧化锝（V）的N2 S2络合物的一般结构使得它们可以取代类固醇的BC环系统，从而产生与类固醇具有相当大的尺寸和形状相似性的金属络合物系统。这样的金属集成类固醇形状的复合物可以构建为两个不同的氨基硫醇的异二聚体;具有这种异二聚体双二齿结构的锝和锝的复合物尚未被系统地研究。在这项调查中，我们已经表明，这种性质的络合物形式容易当适当的金属前体与氨基硫醇的混合物相结合。在我们所研究的体系中，异二聚体复合物的形成优于同二聚体复合物的形成，并且在我们能够获得X射线晶体结构的一个体系中，这种氧合铼异二聚体具有所需的反式几何结构。这些锝和锝-99m络合物对配体交换是相当稳定的，它们可以很容易地通过色谱法在适当的条件下纯化，在体内研究的一个锝-99m络合物在血液中显示出一定的持久性，并在几个组织中提供了良好的初始摄取。这种双二齿异二聚体配合物的方便和选择性的形成表明，类似于受体配体的金属集成配合物的发展是可能的。
We have investigated thepossibility of preparing complexes of rhenium and technetium whose shape resembles that of ligands for steroid receptors. The general structure of N2S2 complexes of oxorhenium (V) and oxotechnetium (V) is such that they could replace the BC ring system of steroid, thereby generating a metal complex system with considerable size and shape similarity to a steroid. Such a metal-integrated steroid-shaped complex can be constructed as a heterodimer of two different amino thiols; complexes of rhenium and technetium with such heterodimeric bis-bidentate structure have not been systematically studied. In this investigation, we have shown that complexes of this nature form readily when appropriate metal precursors are combined with a mixture of amino thiols. In the systems we have studied, heterodimeric complex formation is preferred over homodimeric complex formation, and in one system where we were able toobtain an X-ray crystal structure, this oxorhenium heterodimer had the desired trans geometry. These rhenium and technetium-99m complexes are reasonably stable toward ligand exchange; they can be readily purified by chromatography under appropriate conditions, and the one technetium-99m complex studied in vivo shows some persistence in bloodand gives good initial uptake in several tissues. The convenient and selective formation of such bis-bidentate heterodimeric complexes suggests that the development of metal-integrated complexes that resemble ligands for receptors may be possible.