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一种新型双核铂配合物,其含有一种含氮偕二膦酸酯,作为一种潜在的抗癌化合物,可特异性靶向骨组织。

A new dinuclear platinum complex with a nitrogen-containing geminal bisphosphonate as potential anticancer compound specifically targeted to bone tissues.

作者信息

Margiotta Nicola, Capitelli Francesco, Ostuni Rosa, Natile Giovanni

机构信息

Dipartimento Farmaco-Chimico, Università degli Studi di Bari, via Orabona 4, 70125 Bari, Italy.

出版信息

J Inorg Biochem. 2008 Dec;102(12):2078-86. doi: 10.1016/j.jinorgbio.2008.07.008. Epub 2008 Jul 26.

Abstract

The paper describes the synthesis and characterization of a new platinum dinuclear complex (2) bearing a nitrogen-containing geminal bisphosphonate (NBP, 1), structurally related to the commercial drug risedronate. NBPs themselves have shown in quite a few cases to be endowed with anticancer activity, therefore the new platinum complex has two potential antitumor moieties (the NBP ligand and the platinum residue) and could have high affinity for bone tumors or metastases (due to the presence of NBP). The free bisphosphonate (1) has been crystallized by a sol-gel method and characterized by X-ray diffraction analysis. The platinum complex (2) has been found to have a dinuclear structure with the bisphosphonate bridging two platinum moieties in a W conformation.

摘要

本文描述了一种新型铂双核配合物(2)的合成与表征,该配合物含有与市售药物利塞膦酸盐结构相关的含氮偕二膦酸盐(NBP,1)。在相当多的案例中,NBP本身已显示出具有抗癌活性,因此这种新型铂配合物有两个潜在的抗肿瘤部分(NBP配体和铂残基),并且可能对骨肿瘤或转移瘤具有高亲和力(由于NBP的存在)。游离的双膦酸盐(1)已通过溶胶 - 凝胶法结晶,并通过X射线衍射分析进行了表征。已发现铂配合物(2)具有双核结构,双膦酸盐以W构象桥连两个铂部分。

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