| Full text | |
| Author(s): Show less - |
Rocha, Fillipe V.
[1]
;
Farias, Renan L.
[2]
;
Lima, Mauro A.
[1]
;
Batista, Victor S.
[3]
;
Nascimento-Junior, Nailton M.
[3]
;
Garrido, Saulo S.
[4]
;
Leopoldino, Andrea M.
[5]
;
Goto, Renata N.
[5]
;
Oliveira, Adriano B.
[6]
;
Beck, Johannes
[7]
;
Landvogt, Christian
[7]
;
Mauro, Antonio E.
[2]
;
Netto, Adelino V. G.
[2]
Total Authors: 13
|
| Affiliation: | [1] UFSCar Univ Fed Sao Carlos, Dept Quim, Sao Carlos, SP - Brazil
[2] UNESP Univ Estadual Paulista, Inst Quim, Dept Quim Geral & Inorgan, Araraquara - Brazil
[3] UNESP Univ Estadual Paulista, Inst Quim, Dept Quim Organ, Araraquara - Brazil
[4] UNESP Univ Estadual Paulista, Inst Quim, Dept Bioquim & Tecnol Quim, Araraquara - Brazil
[5] Univ Sao Paulo, Dept Clin Anal Toxicol & Food Sci, Ribeirao Preto - Brazil
[6] Univ Fed Sergipe, Dept Quim, Sao Cristovao - Brazil
[7] Rheinische Friedrich Wilhelms Univ Bonn, Inst Anorgan Chem, Bonn - Germany
Total Affiliations: 7
|
| Document type: | Journal article |
| Source: | Journal of Inorganic Biochemistry; v. 199, OCT 2019. |
| Web of Science Citations: | 7 |
| Abstract | |
Herein, a robust docking protocol was developed by using a low-cost workflow to highlight the modulation at ATPase domain from Human Topoisomerase-Ha (TOP2A) towards four novel Pd(II)-complexes bearing N,S-donor ligands. In vitro TOP2A inhibition assay confirmed the ability of them to prevent the enzyme functions into concentration ranging at 6.25-25 mu M. These results exhibited more effectivity than anticancer agent etoposide (35 mu M) and merbarone (40-50 mu M). The compounds were screened via Resazurin assay against MCF-7, MDA-MB-231 (Human breast), DU-145 (Human prostate), A549 (Human lung) and Ca127 (Human tongue) tumor cell lines revealing great cytotoxic effects, primarily to MCF-7 (IC50 = 1.81-4.46 mu M). As well, 1-4 exhibited their selectivity index (SI) higher than cisplatin against HEK-293 (human kidney) normal cells, at least 11.6-fold = (SI1.4 = 1.4-5.0; Sl(cis) = 0.12). Further, Red Blood Cell hemolytic test suggested in vitro non-toxic character for compound 4, previously evaluated as the most effective TOP2A inhibitor. (AU) | |
| FAPESP's process: | 12/15486-3 - Pd(II) compounds: synthesis, cytotoxicity, and DNA binding studies |
| Grantee: | Regina Celia Galvao Frem |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 16/17711-5 - INVESTIGATION OF THE ANTITUMOR POTENTIAL OF PALLADIUM(II) COMPOUNDS CONTAINING ORTHOMETALLATED OR N,S-DONOR LIGANDS |
| Grantee: | Adelino Vieira de Godoy Netto |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 13/20156-5 - Design of new thiosemicarbazones and their Cu(II) and Pd(II) complexes as topoisomerase inhibitors |
| Grantee: | Fillipe Vieira Rocha |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |
| FAPESP's process: | 16/04201-9 - Transition metal compounds bearinhg thiosemicarbazones and phosphines as ligand: investigation of cytotoxicity and mechanism of action |
| Grantee: | Fillipe Vieira Rocha |
| Support Opportunities: | Regular Research Grants |