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一种新型细胞毒铈配合物:三氯化水合(1,10-菲啰啉)合铈(III)(KP776)。合成、表征、在 H2O 中的行为、与生物分子的结合以及抗增殖活性。

A novel cytotoxic cerium complex: aquatrichloridobis(1,10-phenanthroline)cerium(III) (KP776). Synthesis, characterization, behavior in H2O, binding towards biomolecules, and antiproliferative activity.

机构信息

University of Vienna, Institute of Inorganic Chemistry, Waehringer Strasse 42, A-1090 Vienna.

出版信息

Chem Biodivers. 2009 Dec;6(12):2153-65. doi: 10.1002/cbdv.200900011.

DOI:10.1002/cbdv.200900011
PMID:20020447
Abstract

The lanthanide complex aquatrichloridobis(1,10-phenanthroline)cerium(III) [Ce(phen)2(H2O)Cl3] (KP776) was fully characterized by elemental analysis, IR-, and 1H- and 13C-NMR spectroscopy, as well as TG/DTA measurements, and its behavior in H2O, important for the application as a chemotherapeutic, was studied. In addition, the binding of KP776 to nucleotides and single serum proteins was investigated by capillary electrophoresis, whereas binding to proteins in human plasma was observed by ICP-MS. The compound shows promising anticancer properties in vitro: proliferation of human cancer cell lines is strongly inhibited with IC(50) values in the very low micromolar range.

摘要

镧系元素配合物三氯化水合 1,10-菲啰啉合铈(III) [Ce(phen)2(H2O)Cl3](KP776)通过元素分析、IR 光谱、1H 和 13C-NMR 光谱以及 TG/DTA 测量进行了全面表征,并研究了其在 H2O 中的行为,这对于作为化疗药物的应用很重要。此外,通过毛细管电泳研究了 KP776 与核苷酸和单一血清蛋白的结合,而通过 ICP-MS 观察了其与人血浆蛋白的结合。该化合物在体外具有有前景的抗癌特性:人癌细胞系的增殖受到强烈抑制,IC50 值处于非常低的微摩尔范围内。

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