Crystal structure, anti-Trypanosoma cruzi and cytotoxic activities of Cu(II) complexes bearing β-diketone and α-diimine ligands

[Display omitted] •Three novel Cu(II) complexes containing β-diketone were prepared.•The X-ray structural analysis was performed.•A Cu(II) complex was active and selective toward cancer cell lines.•A Cu(II) complex and its ligand exhibited good activity against T. cruzi. Three novel copper(II) compl...

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Veröffentlicht in:Inorganica Chimica Acta 2020-01, Vol.499, p.119164, Article 119164
Hauptverfasser: Paixão, Drielly A., de Oliveira, Barbara C.A., Almeida, Janaina do Couto, Sousa, Luana M., Lopes, Carla D., Carneiro, Zumira A., Tezuka, Daiane Y., Clavijo, Juan Carlos T., Ellena, Javier, Polloni, Lorena, Machado, Pedro H.A., de Albuquerque, Sérgio, de Oliveira Júnior, Robson J., Guilardi, Silvana, Guerra, Wendell
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Sprache:eng
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Zusammenfassung:[Display omitted] •Three novel Cu(II) complexes containing β-diketone were prepared.•The X-ray structural analysis was performed.•A Cu(II) complex was active and selective toward cancer cell lines.•A Cu(II) complex and its ligand exhibited good activity against T. cruzi. Three novel copper(II) complexes were synthesized: [Cu(tfa)2] (I), [Cu(tfa)(dmb)(NO3)].1.5H2O (II) and [Cu(tfa)(nphen)(NO3)] (III), where tfa = 4,4,4-trifluoro-1-(2-furyl)-1,3-butanedione, nphen = 5-nitro-1,10-phenanthroline and dmb = 4,4-dimethoxy-2,2-bipyridine. They were characterized by elemental analysis, conductivity measurements, FT-IR, UV–Vis and single-crystal X-ray diffraction. The X-ray crystal structures of I, II and III reveal that the β-diketone coordinates via the oxygen atoms, while the heterocyclic bases coordinate via their two nitrogen atoms. The cytotoxic activity of I, II and III was investigated in two tumor cell lines (Ehrlich tumor and sarcoma 180) and in a non-tumor cell line (myoblast C2C12). Complex III exhibited good activity (IC50 Ehrlich = 15.75 μM and IC50 sarcoma 180 = 16.90 μM) and selectivity (SI > 4) in both tumor cell lines. Subsequently, it was found that III also present good activity against Trypanosoma cruzi.
ISSN:0020-1693
1873-3255
DOI:10.1016/j.ica.2019.119164