Synthesis, structure and cytotoxic activity of mixed-valent Cu(I)/Cu(II) salt containing a pyrazolone derivative as ligand

The compound [Cu(TAMEN)][Cu(NCS)2Cl](DMF)2 containing the Mannich base N,N′-tetra-(4-antipyrylmethyl)-1,2-diaminoethane (TAMEN), as ligand, was synthesized and characterized by conductometric, magnetic, electronic and infrared spectroscopic properties. The single-crystal X-ray structure shows the presence of two well defined complex units, [Cu(TAMEN)]2+ and [Cu(NCS)2Cl]2−.The complex cation contains copper(II) in the elongated pseudo-octahedral environment created by the N2O4 donor set of TAMEN whereas, the counterion exhibits a pseudo trigonal planar geometry around the Cu(I) ion.Both, the pyrazolonic ligand and the complex have been screened for their cytotoxic activity against human tumor cell lines: glioblastoma multiforme, breast cancer, hepatoma and lung carcinoma. The nontumor cell lines MDBK (bovine kidney) and BALB/c 3T3 clone 31 (mouse embryo) were also included in the experiments. In contrast to the ligand TAMEN, the [Cu(TAMEN)][Cu(NCS)2Cl](DMF)2 was found to decrease in a time- and concentration-dependent manner the viability of cultured tumor (MCF-7, A549, 8MGBA, Hep G2) and non-tumor (MDBK, BALB/c 3T3) cell lines.

We report in this paper the synthesis, the structure and the cytotoxic activity of [Cu(TAMEN)][Cu(NCS)2Cl](DMF)2 against human tumor cell lines.Figure optionsDownload as PowerPoint slideHighlights
► Structure of [Cu(TAMEN)][Cu(NCS)2Cl](DMF)2 has been resolved by X-ray diffraction.
► There are two well defined complex units, [Cu(TAMEN)]2+ and [Cu(NCS)2Cl]2-.
► Compound decrease in time- and concentration-dependent manner cell lines viability.