Advanced search
Start date
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

Full text
Show less -
de Moura, Thales Reggiani [1] ; Zanetti, Renan Diego [1] ; Silva, Debora Eduarda Soares [1] ; de Farias, Renan Lira [1] ; Mauro, Antonio Eduardo [1] ; Pereira, Jose Clayston Melo [1] ; de Souza, Aline Aparecida [2] ; da Silva Siqueira, Fabio [2] ; de Souza Judice, Wagner Alves [2] ; Lima, Mauro Almeida [3] ; Rocha, Fillipe Vieira [3] ; Deflon, Victor Marcelo [4] ; Vieira de Godoy Netto, Adelino [1]
Total Authors: 13
[1] UNESP Univ Estadual Paulista, Inst Quim, Dept Quim Geral & Inorgan, BR-14800060 Araraquara, SP - Brazil
[2] UMC Univ Mogi das Cruzes, Ctr Interdisciplinar Invest Bioquim, BR-08701970 Mogi Das Cruzes, SP - Brazil
[3] UFSCar Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Sao Paulo, Inst Quim Sao Carlos, BR-13566590 Sao Carlos, SP - Brazil
Total Affiliations: 4
Document type: Journal article
Source: NEW JOURNAL OF CHEMISTRY; v. 44, n. 45, p. 19891-19901, DEC 7 2020.
Web of Science Citations: 0

Four palladium(ii) compounds of general formulae {[}PdCl(L-n)(PPh3)] [L-1 = 3,5-dimethylpyrazole-1-iminothiolate (1); L-2 = 3,5-dimethyl-pyrazole-N-methyl-1-iminothiolate (2); L-3 = 3,5-dimethylpyrazole-N-ethyl-1-iminothiolate (3); L-4 = 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 (H-1 and C-13) 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 2 and 3 to ct-DNA have been studied using circular dichroism and fluorescence spectroscopy. The topoisomerase II alpha 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 mu M. Docking simulations have been carried out to gain more information about the interaction of the complexes and cathepsin B. (AU)

FAPESP's process: 15/12098-0 - Dinitrosyl complexes containing thiol and/or thiosemicarbazone : synthesis, characterization and treatment against cancer
Grantee:José Clayston Melo Pereira
Support type: Regular Research Grants
FAPESP's process: 16/25112-4 - Evaluation of modulators of the activity of proteases involved in pathological processes
Grantee:Wagner Alves de Souza Júdice
Support type: Regular Research Grants
FAPESP's process: 14/02205-1 - Study of kinetic behavior of convertases
Grantee:Wagner Alves de Souza Júdice
Support type: Regular Research Grants
FAPESP's process: 09/54011-8 - Acquisition of a single-crystal X-ray diffractometer for the structural analysis of small molecules and proteins
Grantee:Victor Marcelo Deflon
Support type: Multi-user Equipment Program
FAPESP's process: 19/11242-1 - Relative quantification of DNA-Topoisomerases enzymes in cell lines: Correlation between cytotoxicity and mechanism of action of coordination compounds
Grantee:Fillipe Vieira Rocha
Support type: Regular Research Grants
Grantee:Adelino Vieira de Godoy Netto
Support type: Regular Research Grants