Synthesis, characterization, cytotoxicity study, interaction with DNA and topoisomerase IIα of square-planar complexes with thiosemicarbazones

被引：2

作者：

Silva, Ludimila Thayane Paes ^{[1
,2
]}

Pereira, George Bueno Santana ^{[1
]}

de Oliveira, Gabriela Porto ^{[1
]}

Lima, Mauro Almeida ^{[1
]}

de Araujo Neto, Joao Honorato ^{[3
]}

Akinyemi, Amos Olalekan ^{[4
]}

Vieira, Marcelle Alcantara ^{[5
]}

Nascimento-Junior, Nailton Monteiro ^{[5
]}

de Farias, Renan Lira ^{[6
]}

Ellena, Javier Alcides ^{[7
]}

de Godoy Netto, Adelino Vieira ^{[8
]}

Rocha, Fillipe Vieira ^{[1
]}

机构：

[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP, Brazil

[2] Inst Fed Educ, Ciencia & Tecnol Baiano, Campus Guanambi, Guanambi BR-46430000, BA, Brazil

[3] Univ Sao Paulo, Dept Quim Fundamental, Inst Quim, BR-05508900 Sao Paulo, SP, Brazil

[4] Univ Kentucky, Dept Toxicol & Canc Biol, Lexington, KY USA

[5] Univ Estadual Paulista, Dept Bioquim & Quim Organ, Inst Quim, BR-14800060 Araraquara, RJ, Brazil

[6] Pontificia Univ Catolica Rio de Janeiro, Dept Elect Engn, BR-22453900 Rio De Janeiro, RJ, Brazil

[7] Univ Sao Paulo, Inst Fis Sao Carlos, BR-13566590 Sao Carlos, SP, Brazil

[8] UNESP Univ Estadual Paulista, Dept Quim Geral & Inorgan, Inst Quim Araraquara, BR-14801970 Araraquara, SP, Brazil

来源：

POLYHEDRON | 2024年 / 257卷

基金：

巴西圣保罗研究基金会;

关键词：

ct-DNA; Topoisomerase; Cytotoxicity; Thiosemicarbazone; Palladium(II); Nickel(II); PALLADIUM(II) COMPLEXES; PLATINUM(II) COMPLEXES; PD(II) COMPLEXES; DFT CALCULATIONS; BINDING; CLEAVAGE; DESIGN;

D O I：

10.1016/j.poly.2024.117021

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

In this study, we report the synthesis and characterization of eight new palladium complexes and a nickel complex containing thiosemicarbazone ligands derived from chalcones and benzalketones. The techniques of Infrared and UV-visible spectroscopy, Nuclear Magnetic Resonance, Mass Spectrometry, and Elemental Analysis fully characterized the compounds. Crystallography was successful for five complexes and two ligands, allowing for X-ray Diffraction analysis. Molecular docking studies and assays involving DNA interaction via agarose gel electrophoresis and UV-Vis titration revealed no DNA interaction or inhibition of topoisomerase II alpha enzyme activity. However, these compounds demonstrated potent cytotoxic effects (IC50) against breast tumor (MCF-7) and prostate (DU-145) cell lines, as well as non-tumor prostate (PNT2) cell lines. These findings highlight the relevance of structural variations and the metallic center's nature in achieving cytotoxic effects, offering insights into the development of bioactive compounds.

引用

页数：9

共 45 条

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