Abstract
The focus of this research is on the study of a series of copper (II) benzoylpyridine thiosemicarbazone complexes. Of the six benzoylpyridine thiosemicarbazone ligands used in this study, two are reported for the first time; 2-benzoylpyridine tert-butyl thiosemicarbazone (BZP-tBTSC), and 2-benzoylpyridine benzyl thiosemicarbazone (BZP-BzTSC). Once characterized by NMR, melting point, and MS, these mono-anionic tridentate ligands were then reacted with Cu2+ to form the new square planar metal complexes [Cu(BZP-tBTSC)Cl] and [Cu(BZP-BzTSC)Cl]. All of the copper complexes display marked inhibition of human topoisomerase IIα. The [Cu(BZP-tBTSC)Cl] complex shows marked activity against human breast cancer cell lines.
Highlights
Thiosemicarbazones are an interesting class of chemical compounds that have active biological and medicinalHow to cite this paper: Conner, J.D., et al (2016) Cu(II) Benzoylpyridine Thiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells
Copper(II) complexes of the BZP-TSC ligands synthesized from copper (II) chloride are paramagnetic square-planar complexes in solution as has been determined previously, and we find evidence that the [Cu(BZP-tBTSC)Cl] and the [Cu(BZP-BzTSC)Cl] have the same solution structure
Thiosemicarbazones that are of the α-(N)-heterocyclic thiosemicarbazone class, such as the BZP-TSC’s in this study, have proven to be a special class of ligands with many biological properties
Summary
Thiosemicarbazones are an interesting class of chemical compounds that have active biological and medicinalHow to cite this paper: Conner, J.D., et al (2016) Cu(II) Benzoylpyridine Thiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells. These compounds act as ligands for a wide variety of transition metals, often as high affinity multi-dentate chelating agents [1] [6] [7]. A specific subset of thiosemicarbazone ligands that have been referred to as α-(N)-heterocyclic thiosemicarbazones have potent antiproliferative properties against a wide variety of microbes and cancer cells. Α-N-heterocyclic thiosemicarbazones, with their N-N-S tridentate coordination backbone, are well-known for their ability to chelate to biologically important transition metals, such as Cu(II) and Fe(II) [14]-[18]
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