Palladium(ii) complexes bearing 1-iminothiolate-3,5-dimethylpyrazoles: Synthesis, cytotoxicity, DNA binding and enzymatic inhibition studies

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorUniversidade Estadual Paulista (Unesp)-
Autor(es): dc.contributorCentro Interdisciplinar de Investigação Bioquímica-
Autor(es): dc.contributorUniversidade Federal de São Carlos (UFSCar)-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.creatorDe Moura, Thales Reggiani [UNESP]-
Autor(es): dc.creatorZanetti, Renan Diego [UNESP]-
Autor(es): dc.creatorSilva, Debora Eduarda Soares [UNESP]-
Autor(es): dc.creatorDe Farias, Renan Lira [UNESP]-
Autor(es): dc.creatorMauro, Antonio Eduardo [UNESP]-
Autor(es): dc.creatorPereira, José Clayston Melo [UNESP]-
Autor(es): dc.creatorDe Souza, Aline Aparecida-
Autor(es): dc.creatorDa Silva Siqueira, Fábio-
Autor(es): dc.creatorDe Souza Júdice, Wagner Alves-
Autor(es): dc.creatorLima, Mauro Almeida-
Autor(es): dc.creatorRocha, Fillipe Vieira-
Autor(es): dc.creatorDeflon, Victor Marcelo-
Autor(es): dc.creatorDe Godoy Netto, Adelino Vieira [UNESP]-
Data de aceite: dc.date.accessioned2022-02-22T00:48:35Z-
Data de disponibilização: dc.date.available2022-02-22T00:48:35Z-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2020-12-06-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1039/d0nj02825h-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/206903-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/206903-
Descrição: dc.descriptionFour palladium(ii) compounds of general formulae [PdCl(Ln)(PPh3)] {L1 = 3,5-dimethylpyrazole-1-iminothiolate (1); L2 = 3,5-dimethyl-pyrazole-N-methyl-1-iminothiolate (2); L3 = 3,5-dimethylpyrazole-N-ethyl-1-iminothiolate (3); L4 = 3,5-dimethylpyrazole-N-phenyl-1-iminothiolate (4); and PPh3 = triphenylphosphine} have been synthesized. The novel synthesized compounds have been characterized by C, H and N elemental analysis, 1D (1H and 13C) and 2D (HSQC and HMBC) NMR, MS, FT-IR, and molar electrical conductivity measurements. The molecular structure of complex 3 has been solved by single-crystal X-ray crystallography. The stability of the complexes in solution was studied in a DMSO/D2O (7 : 3) solution after 48 h. The antiproliferative activity of all free ligands and the stable palladium complexes 2-4 was assayed using the human breast tumour cell line MCF-7, lung tumour cell line A549 and human fetal lung fibroblast cell line MRC-5. Complex 3 was more active than cisplatin against MCF-7 cells, whilst palladium compounds 2-4 exhibited no drug response towards A549 cells at concentrations <50 μM. The binding properties of compounds 2 and 3 to ct-DNA have been studied using circular dichroism and fluorescence spectroscopy. The topoisomerase IIα inhibition has been studied for complex 2 and 3. The ability of all complexes to inhibit the activity of cathepsin B and L has also been investigated in this work. Compound 4 inhibited more than 50% of the cathepsin B activity at a concentration of 10 μM. Docking simulations have been carried out to gain more information about the interaction of the complexes and cathepsin B.-
Descrição: dc.descriptionUNESP-Univ. Estadual Paulista Instituto de Química Departamento de Química Geral e Inorgânica-
Descrição: dc.descriptionUMC - Univ. de Mogi das Cruzes Centro Interdisciplinar de Investigação Bioquímica-
Descrição: dc.descriptionUFSCar-Univ. Federal de São Carlos Departamento de Química-
Descrição: dc.descriptionUSP-Univ. de São Paulo Instituto de Química de São Carlos-
Descrição: dc.descriptionUNESP-Univ. Estadual Paulista Instituto de Química Departamento de Química Geral e Inorgânica-
Formato: dc.format19891-19901-
Idioma: dc.languageen-
Relação: dc.relationNew Journal of Chemistry-
???dc.source???: dc.sourceScopus-
Título: dc.titlePalladium(ii) complexes bearing 1-iminothiolate-3,5-dimethylpyrazoles: Synthesis, cytotoxicity, DNA binding and enzymatic inhibition studies-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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