Quinoline-2-carboxaldehyde thiosemicarbazones and their Cu(II) and Ni(II) complexes as topoisomerase IIa inhibitors

Journal of Inorganic Biochemistry
Franco BisceglieG Pelosi

Abstract

A series of quinoline-2-carboxaldehyde thiosemicarbazones and their copper(II) and nickel(II) complexes were synthesized and characterized. In all complexes the ligands are in the E configuration with respect to the imino bond and behave as terdentate. The copper(II) complexes form square planar derivatives with one molecule of terdentate ligand and chloride ion. A further non-coordinated chloride ion compensates the overall charge. Nickel(II) ions form instead octahedral complexes with two ligands for each metal ion, independently from the stoichiometric metal:ligand ratio used in the synthesis. Ligands and complexes were tested for their antiproliferative properties on histiocytic lymphoma cell line U937. Copper(II) derivatives are systematically more active than the ligands and the nickel complexes. All copper derivatives result in inhibiting topoisomerase IIa in vitro. Computational methods were used to propose a model to explain the different extent of inhibition presented by these compounds. The positive charge of the dissociated form of the copper complexes may play a key role in their action.

References

Dec 11, 1999·Nucleic Acids Research·H M BermanP E Bourne
Feb 3, 2004·Mini Reviews in Medicinal Chemistry·Heloisa Beraldo, Dinorah Gambino
Jul 21, 2004·Journal of Computational Chemistry·Eric F PettersenThomas E Ferrin
Aug 16, 2005·The Journal of Biological Chemistry·Hua WeiGregory L Verdine
Feb 7, 2006·Journal of Molecular Graphics & Modelling·Junmei WangDavid A Case
Aug 13, 2010·Metallomics : Integrated Biometal Science·Joseph E Deweese, Neil Osheroff
Sep 1, 2009·Future Medicinal Chemistry·Danuta S KalinowskiDes R Richardson
Oct 14, 2014·Metallomics : Integrated Biometal Science·Nasma D EljackRonald J Clarke

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Citations

Mar 17, 2016·Chemical Research in Toxicology·James T WilsonJoseph E Deweese
Oct 30, 2019·Mini Reviews in Medicinal Chemistry·Bhushan Shakya, Paras Nath Yadav
Nov 15, 2016·Metallomics : Integrated Biometal Science·Franco BisceglieGiorgio Pelosi

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