A Tridentate Cu(II) Complex with a 2-(4′-Aminophenyl)Benzothiazole Derivative: Crystal Structure and Biological Evaluation for Anticancer Activity

Herein, the synthesis, structural characterization and in vitro biological evaluation of a novel Cu(II) complex with the 2-(4-aminophenyl)benzothiazole pharmacophore conjugated with the (2-pyridinyl)methylamino chelating moiety is reported for the first time. A full characterization of the Cu(II) co...

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Published inInorganics Vol. 11; no. 3; p. 132
Main Authors Mavroidi, Barbara, Sagnou, Marina, Halevas, Eleftherios, Mitrikas, George, Kapiris, Fotis, Bouziotis, Penelope, Hatzidimitriou, Antonios G., Pelecanou, Maria, Methenitis, Constantinos
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 01.03.2023
Subjects
2-(4-aminophenyl)benzothiazole
Anticancer properties
Antitumor activity
Apoptosis
Benzothiazole
Biological activity
Cancer
Cell cycle
Chelation
Circular dichroism
Clinical trials
Copper
copper(II) complex
Crystal structure
Crystallography
Cytotoxicity
Dichroism
DNA binding studies
Ethidium bromide
Fibroblasts
Glioblastoma
in vitro evaluation
Intracellular
Ligands
Lung cancer
Nitrates
Nitrogen
Palladium
Prostate
Prostate cancer
Spectroscopy
Spectrum analysis
Structural analysis
Thermal denaturation
Toxicity
Tumor cell lines
Viscometry
X-ray crystallography
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Summary:Herein, the synthesis, structural characterization and in vitro biological evaluation of a novel Cu(II) complex with the 2-(4-aminophenyl)benzothiazole pharmacophore conjugated with the (2-pyridinyl)methylamino chelating moiety is reported for the first time. A full characterization of the Cu(II) complex was conducted by X-ray crystallography, EPR, IR, elemental and MS analysis, and its binding to CT-DNA was investigated by UV-vis spectroscopy, ethidium bromide competition studies, circular dichroism, viscometry and thermal denaturation. The data clearly indicate that the Cu(II) complex interacts with CT-DNA via intercalation, registering a difference compared to previously reported Pt(II) and Pd(II) analogues. To evaluate the anticancer activity of the complex, a series of in vitro experiments against breast, glioblastoma, prostate and lung cancer cell lines along with healthy fibroblasts were implemented. Cytotoxicity, cellular uptake, intracellular ROS production, cell cycle and apoptosis analysis revealed an increased anticancer activity towards breast cancer cells that is accompanied by an induction in intracellular ROS levels and a significant G2/M arrest followed by apoptosis.
ISSN:2304-6740
2304-6740
DOI:10.3390/inorganics11030132