4.5 Article

New BI and TRI-Thiazole copper (II) complexes in the search of new cytotoxic drugs against breast cancer cells

期刊

INORGANICA CHIMICA ACTA
卷 508, 期 -, 页码 -

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ELSEVIER SCIENCE SA
DOI: 10.1016/j.ica.2020.119622

关键词

Copper complexes; Thiazoles; X-ray diffraction; Cytotoxicity; Breast cancer

资金

  1. PEDECIBA Quimica (Uruguayan research funding Program)
  2. PECECIBA Biologia (Uruguayan research funding Program)

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New thiazolyl derivatives (BT and TT) and their copper (II) complexes [Cu2Cl2(BT)(2)] (Cu-BT) and [Cu4ClO2(TT)(2)]PF6 center dot 3.5H(2)O (Cu-TT) were synthesized and characterized by elemental analysis, H-1 NMR and C-13 NMR, HRMS, X-ray diffraction, IR and UV-Vis spectroscopies. The crystal structure of Cu-BT shows the formation of a dinuclear complex where each copper(II) center is bonded to two thiazol N atoms, from different BT ligands, one deprotonated amide N atom, an O atom from the ester terminal groups and a chlorine atom. The structure found for Cu-TT is a positively charged tetranuclear moiety containing two deprotonated TT ligands, a chlorine anion, two hydroxide anions acing as bridges between the copper centers and a water molecule. The cytotoxic activity of both copper complexes was evaluated on metastatic breast cancer cell lines, characterized for its rapidly dividing behavior. Both, Cu-BT and Cu-TT, show higher cytotoxic activity against these tumor cells than free BT and TT and also than cisplatin. In addition, we found that both complexes interact with DNA. Consistently, they also show cytotoxicity against a rapidly dividing non-tumor cell line, although with higher IC50, being such interaction and selectivity an indicator of the possible coexistence of more than one mechanism of action.

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