Alexandre B. de Carvalho, Marcos V. Palmeira-Mello, Paulo N. de Souza, Saulo H. Mendes Abe, José Balena G. Filho, Marcelo B. Andrade, Rodrigo S. Corrêa, Alzir A. Batista, Javier Ellena,
Five novel heteroleptic copper(II) complexes were synthesized and fully characterized. Unlike previously reported Cu(II)-diimine systems, these complexes incorporate an O,O-chelating 5-chloro-2-hydroxybenzophenone (5-Cl2HBz) ligand, forming cytotoxic compounds active against A2780 (ovarian), A549 (lung), and MCF-7 (breast) cancer cells. The complexes were identified as [Cu(5-Cl2HBz)(phen)(NO3)] (Cu(1)), [Cu(5-Cl2HBz)(bathophen)](NO3)1.5H2O·CH3OH (Cu(2)), [Cu(5-Cl2HBz)(bipy)(NO3)(H2O)] (Cu(3)), [Cu(5-Cl2HBz)(5,5′-bipy)(NO3)] (Cu(4)), and [Cu(5-Cl2HBz)(tert-bipy)(NO3)]·2H2O (Cu(5)), where phen = 1,10-phenanthroline, bathophen = 4,7-diphenyl-1,10-phenanthroline, bipy = 2,2′-bipyridine, 5,5′-bipy = 5,5′-bipyridine, and tert-bipy = 4,4′-bis(tert-butyl)-2,2′-bipyridine. Among the series, complex Cu(2) displayed outstanding potency in A2780 cells (IC50 = 0.24 μM), being 36-fold more potent than cisplatin. This complex significantly affected the cell morphology and colony formation in a concentration-dependent manner. DNA interaction studies revealed that Cu(2) interacts strongly with DNA, as evidenced by viscosity, circular dichroism, and fluorescence measurements. These findings establish Cu(II)-bathophen derivatives as highly promising candidates for the development of copper-based anticancer agents.
https://doi.org/10.1021/acsomega.5c11889
@article{B_de_Carvalho_2026, title={Copper(II)-5-chloro-2-hydroxybenzophenone Complexes with N – N Donors: Structural Insights and Antitumor Activity against A2780 Human Ovarian Cancer Cells of a Bathophen Derivative}, volume={11}, ISSN={2470-1343}, url={http://dx.doi.org/10.1021/acsomega.5c11889}, DOI={10.1021/acsomega.5c11889}, number={10}, journal={ACS Omega}, publisher={American Chemical Society (ACS)}, author={B. de Carvalho, Alexandre and Palmeira-Mello, Marcos V. and de Souza, Paulo N. and Mendes Abe, Saulo H. and Balena G. Filho, José and Andrade, Marcelo B. and Corrêa, Rodrigo S. and Batista, Alzir A. and Ellena, Javier}, year={2026}, month=mar, pages={16321–16332} }