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dc.contributor.author
Rada, Jesica Paola
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Bastos, Beatriz S. M.
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Anselmino Dieterle, Luciano Emanuel
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Franco, Chris H. J.
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Lanznaster, Mauricio
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Diniz, Renata
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Fernandez, Claudio Oscar
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Menacho Márquez, Mauricio Ariel
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Percebom, Ana Maria
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Rey, Nicolás A.
dc.date.available
2021-12-30T17:59:06Z
dc.date.issued
2019-07
dc.identifier.citation
Rada, Jesica Paola; Bastos, Beatriz S. M.; Anselmino Dieterle, Luciano Emanuel; Franco, Chris H. J.; Lanznaster, Mauricio; et al.; Binucleating Hydrazonic Ligands and Their μ-Hydroxodicopper(II) Complexes as Promising Structural Motifs for Enhanced Antitumor Activity; American Chemical Society; Inorganic Chemistry; 58; 13; 7-2019; 8800-8819
dc.identifier.issn
0020-1669
dc.identifier.uri
http://hdl.handle.net/11336/149470
dc.description.abstract
Very few inorganic antineoplastic drugs have entered the clinic in the last decades, mainly because of toxicity issues. Because copper is an essential trace element of ubiquitous occurrence, decreased side effects could be expected in comparison with the widely used platinum anticancer compounds. In the present work, two novel hydrazonic binucleating ligands and their μ-hydroxo dicopper(II) complexes were prepared and fully characterized. They differ by the nature of the aromatic group present in their aroylhydrazone moieties: while H3L1 and its complex, 1, possess a thiophene ring, H3L2 and 2 contain the more polar furan heterocycle. X-ray diffraction indicates that both coordination compounds are very similar in structural terms and generate dimeric arrangements in the solid state. Positive-ion electrospray ionization mass spectrometry analyses confirmed that the main species present in a 10% dimethyl sulfoxide (DMSO)/water solution should be [Cu2(HL)(OH)]+ and the DMSO-substituted derivative [Cu2(L)(DMSO)]+. Scattering techniques [dynamic light scattering (DLS) and small-angle X-ray scattering] suggest that the complexes and their free ligands interact with bovine serum albumin (BSA) in a reversible manner. The binding constants to BSA were determined for the complexes through fluorescence spectroscopy. Moreover, to gain insight into the mechanism of action of the compounds, calf thymus DNA binding studies by UV-visible and DLS measurements using plasmid pBR322 DNA were also performed. For the complexes, DLS data seem to point to the occurrence of DNA cleavage to Form III (linear). Both ligands and their dicopper(II) complexes display potent antiproliferative activity in a panel of four cancer cell lines, occasionally even in the submicromolar range, with the complexes being more potent than the free ligands. Our data on cellular models correlate quite well with the DNA interaction experiments. The results presented herein show that aroylhydrazone-derived binucleating ligands, as well as their dinuclear μ-hydroxodicopper(II) complexes, may represent a promising structural starting point for the development of a new generation of highly active potential antitumor agents.
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application/pdf
dc.language.iso
eng
dc.publisher
American Chemical Society
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
μ-Hydroxodicopper(II)
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DNA
dc.subject.classification
Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Binucleating Hydrazonic Ligands and Their μ-Hydroxodicopper(II) Complexes as Promising Structural Motifs for Enhanced Antitumor Activity
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info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
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info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-11-30T15:24:47Z
dc.journal.volume
58
dc.journal.number
13
dc.journal.pagination
8800-8819
dc.journal.pais
Estados Unidos
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dc.journal.ciudad
Washington D. C.
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Fil: Rada, Jesica Paola. Pontifícia Universidade Católica do Rio de Janeiro; Brasil
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Fil: Bastos, Beatriz S. M.. Pontifícia Universidade Católica do Rio de Janeiro; Brasil
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Fil: Anselmino Dieterle, Luciano Emanuel. Universidad Nacional de Rosario. Centro de Estudios Interdisciplinarios. Laboratorio Max Planck de Biología Estructural, Química y Biofísica Molecular de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Investigaciones para el Descubrimiento de Fármacos de Rosario. Universidad Nacional de Rosario. Instituto de Investigaciones para el Descubrimiento de Fármacos de Rosario; Argentina
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Fil: Franco, Chris H. J.. Universidade Federal de Juiz de Fora; Brasil
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Fil: Lanznaster, Mauricio. Universidade Federal Fluminense; Brasil
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Fil: Diniz, Renata. Universidade Federal de Minas Gerais; Brasil
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Fil: Fernandez, Claudio Oscar. Universidad Nacional de Rosario. Centro de Estudios Interdisciplinarios. Laboratorio Max Planck de Biología Estructural, Química y Biofísica Molecular de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Investigaciones para el Descubrimiento de Fármacos de Rosario. Universidad Nacional de Rosario. Instituto de Investigaciones para el Descubrimiento de Fármacos de Rosario; Argentina
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Fil: Menacho Márquez, Mauricio Ariel. Universidad Nacional de Rosario. Centro de Estudios Interdisciplinarios. Laboratorio Max Planck de Biología Estructural, Química y Biofísica Molecular de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Inmunología Clinica y Experimental de Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Médicas. Instituto de Inmunología Clinica y Experimental de Rosario; Argentina
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Fil: Percebom, Ana Maria. Universidade Federal de Minas Gerais; Brasil
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Fil: Rey, Nicolás A.. Pontifícia Universidade Católica do Rio de Janeiro; Brasil
dc.journal.title
Inorganic Chemistry
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/acs.inorgchem.9b01195
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/acs.inorgchem.9b01195
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