Biological activities of polypyridyl-type ligands: implications for bioinorganic chemistry and light-activated metal complexes.

Biological activities of polypyridyl-type ligands: implications for bioinorganic chemistry and light-activated metal complexes.
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多吡啶基型配体的生物学活性:对生物无机化学和光激活金属络合物的影响。

DOI:
10.1016/j.cbpa.2021.01.016
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发表时间:
2021-04
影响因子:
7.8
通讯作者:
Glazer EC
Glazer EC
中科院分区:
生物学2区
文献类型:
--
作者:
Hachey AC;Havrylyuk D;Glazer EC

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多吡啶配位体在药物无机化学中的金属配合物中很常见。这些配体具有内在的细胞毒性,但关于这种现象的详细数据很少,细胞毒性值变化很大,往往是不可重现的。为了提供新的见解的生物效应的联吡啶类配体和结构相关的金属结合系统,报告游离配体细胞毒性进行了审查。25个2,2 ′-联吡啶和1,10-邻菲咯啉衍生物的细胞毒性表明,如NMR位移所示,IC 50值与配体性质如pKa、log D、极化率体积和电子密度之间没有相关性。由于这些观察结果,以及各种报道的多吡啶配体的作用机制,我们提供的假设,生物效应是由实验模型内的特定金属离子的可用性和亲和力。
Polypyridyl coordinating ligands are common in metal complexes used in medicinal inorganic chemistry. These ligands possess intrinsic cytotoxicity, but detailed data on this phenomenon is sparse, and cytotoxicity values vary widely and are often irreproducible. In order to provide new insights into the biological effects of bipyridyl type ligands and structurally related metal-binding systems, reports of free ligand cytotoxicity were reviewed. The cytotoxicity of 25 derivatives of 2,2′-bipyridine and 1,10-phenanthroline demonstrates that there is no correlation between IC50 values and ligand properties such as pKa, log D, polarizability volume, and electron density, as indicated by NMR shifts. As a result of these observations, as well as the various reported mechanisms of action of polypyridyl ligands, we offer the hypothesis that biological effects are governed by the availability of and affinity for specific metal ions within the experimental model.
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