Institute of Inorganic Chemistry, University of Vienna, Währinger Straße 42, 1090, Vienna, Austria.
Research Cluster "Translational Cancer Therapy Research", Währinger Straße 42, 1090, Vienna, Austria.
Chemistry. 2023 Jan 18;29(4):e202202648. doi: 10.1002/chem.202202648. Epub 2022 Nov 29.
A series of six highly lipophilic Cp-substituted molybdenocenes bearing different bioactive chelating ligands was synthesized and characterized by NMR spectroscopy, mass spectrometry and X-ray crystallography. In vitro experiments showed a greatly increased cytotoxic potency when compared to the non-Cp-substituted counterparts. In vivo experiments performed with the dichlorido precursor, (Ph C-Cp) MoCl and the in vitro most active complex, containing the thioflavone ligand, showed an inhibition of tumour growth. Proteomic studies on the same two compounds demonstrated a significant regulation of tubulin-associated and mitochondrial inner membrane proteins for both compounds and a strong metabolic effect of the thioflavone containing complex.
合成并通过 NMR 光谱、质谱和 X 射线晶体学对一系列六种具有不同生物活性螯合配体的高度亲脂性 Cp 取代的钼配合物进行了表征。与非 Cp 取代的对应物相比，体外实验显示出极大地增加了细胞毒性效力。用二氯代前体（Ph C-Cp）MoCl 和体外最活跃的配合物（含硫代黄酮配体）进行的体内实验表明抑制了肿瘤生长。对相同的两种化合物进行的蛋白质组学研究表明，两种化合物的微管相关蛋白和线粒体内膜蛋白均受到显著调节，并且含硫代黄酮的配合物具有强烈的代谢作用。
