TY - JOUR
T1 - Synthesis, characterization, antioxidant potential, and cytotoxicity screening of new Cu(II) complexes with 4-(arylchalcogenyl)-1H-pyrazoles ligands
AU - Pinheiro, Adriana C.
AU - Busatto, Franciele F.
AU - Schaefer, Bruna T.
AU - Tomasini, Paula P.
AU - Nunes, Ianka J.
AU - Machado, Tamara Dos S.
AU - Cargnelutti, Roberta
AU - de Aquino, Thalita F.B.
AU - Ferreira, Kethlin De Q.
AU - Casaril, Angela M.
AU - Jacob, Raquel G.
AU - Savegnago, Lucielli
AU - Hartwig, Daniela
AU - Saffi, Jenifer
N1 - Publisher Copyright:
© 2022 Elsevier Inc.
PY - 2022/12
Y1 - 2022/12
N2 - Two new Cu(II) complexes based on 4-(arylchalcogenyl)-1H-pyrazoles monodentate bis(ligand) containing selenium or sulfur groups (2a and 2b) have been synthesized and characterized by IR spectroscopy, high-resolution mass spectrometry (HRMS), and by X-ray crystallography. In the effort to propose new applications for the biomedical area, we evaluated the antioxidant activity and cytotoxicity of the newly synthesized complexes. The antioxidant activity of the Cu(II) complexes (2a – 2b) were assessed through their ability to inhibit the formation of reactive species (RS) induced by sodium azide and to scavenge the synthetic radicals 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS+). Both copper complexes containing selenium (2a) and sulfur (2b) presented in vitro antioxidant activity. The (1a – 1b and 2a – 2b) compounds did not show cytotoxicity in V79 cells at low concentrations. Furthermore, the antiproliferative activity of free ligands (1a – 1b) and their complexes (2a – 2b) were tested against two human tumor cell lines: MCF-7 (breast adenocarcinoma) and HepG2 (hepatocarcinoma). Also, 2a was tested against U2OS (osteosarcoma). Our results demonstrated that 1a and 1b show little or no growth inhibition activities on human cell lines.The 2a compound exhibited good cytotoxic activity toward human tumor cell lines. However, 2a showed no selectivity, with a selectivity index of 1.12–1.40. Complex 2b was selective for the MCF-7 human tumor cell lines with IC50 of 59 ± 2 μM. This study demonstrates that the Cu(II) complexes 2a and 2b represent promising antitumoral compounds, and further studies are necessary to understand the molecular mechanisms of these effects.
AB - Two new Cu(II) complexes based on 4-(arylchalcogenyl)-1H-pyrazoles monodentate bis(ligand) containing selenium or sulfur groups (2a and 2b) have been synthesized and characterized by IR spectroscopy, high-resolution mass spectrometry (HRMS), and by X-ray crystallography. In the effort to propose new applications for the biomedical area, we evaluated the antioxidant activity and cytotoxicity of the newly synthesized complexes. The antioxidant activity of the Cu(II) complexes (2a – 2b) were assessed through their ability to inhibit the formation of reactive species (RS) induced by sodium azide and to scavenge the synthetic radicals 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS+). Both copper complexes containing selenium (2a) and sulfur (2b) presented in vitro antioxidant activity. The (1a – 1b and 2a – 2b) compounds did not show cytotoxicity in V79 cells at low concentrations. Furthermore, the antiproliferative activity of free ligands (1a – 1b) and their complexes (2a – 2b) were tested against two human tumor cell lines: MCF-7 (breast adenocarcinoma) and HepG2 (hepatocarcinoma). Also, 2a was tested against U2OS (osteosarcoma). Our results demonstrated that 1a and 1b show little or no growth inhibition activities on human cell lines.The 2a compound exhibited good cytotoxic activity toward human tumor cell lines. However, 2a showed no selectivity, with a selectivity index of 1.12–1.40. Complex 2b was selective for the MCF-7 human tumor cell lines with IC50 of 59 ± 2 μM. This study demonstrates that the Cu(II) complexes 2a and 2b represent promising antitumoral compounds, and further studies are necessary to understand the molecular mechanisms of these effects.
KW - Anticancer activity
KW - Antioxidant activities
KW - Copper complexes
KW - Cytotoxicity activity
KW - Organochalcogen
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U2 - 10.1016/j.jinorgbio.2022.112013
DO - 10.1016/j.jinorgbio.2022.112013
M3 - Article
C2 - 36183642
AN - SCOPUS:85138835499
SN - 0162-0134
VL - 237
JO - Journal of Inorganic Biochemistry
JF - Journal of Inorganic Biochemistry
M1 - 112013
ER -