Complexes of N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid with group 12 metals and vanadium—Synthesis, structure and bioactivity of the vanadium complex

• Four metal complexes based on the ligand N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid
• Inhibition of protein tyrosine phosphatase 1B by the vanadium(IV) complex was demonstrated.
• Favorable cytotoxicity of the vanadium(IV) complex in a multidrug-resistant cancer cell line

Four new complexes of group 12 metals [Zn(II), Cd(II) and Hg(II)], along with vanadyl bound to the ligand N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid, have been synthesized and characterized. The structure of the complexes with Zn(II), Hg(II) and V(IV) was determined by X-ray structural analysis. In all observed cases, the symmetry of these complexes was found to be distorted octahedral. The inhibition of protein tyrosine phosphatase 1B by the vanadium(IV) complex was demonstrated. The cytotoxicity of the vanadium(IV) complex was tested in vitro against three cancer cell lines, with a comparison of the activity of the free ligand and of vanadyl acetylacetonate and sodium orthovanadate. The IC50 values of the complex were in the range of 9 to 21 μM. Remarkably, cytotoxic potency in the multidrug-resistant non-small cell lung cancer cell line A549 was at least as high as in the broadly chemosensitive ovarian teratocarcinoma cell line CH1(PA-1).

Four complexes of group 12 metals, along with vanadyl bound to the ligand N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid have been synthesized and characterized. Measurement of cytotoxic activity of the vanadium complex (4) via an MTT assay was performed in three cancer cell lines and highest activity was observed in a multidrug-resistant cell line.Figure optionsDownload as PowerPoint slide