4.7 Article

Mixed Valence Copper(I,II) Binuclear Complexes with Unexpected Structure: Synthesis, Biological Properties and Anticancer Activity

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 14, Pages 6252-6258

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm500154f

Keywords

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Funding

  1. Russian Foundation for Basic Research [12-03-33148, 12-04-00988-a, 14-04-01092-a]
  2. PNR [5.13]
  3. International Associated Laboratory LIA-NUCPROT (CNRS-Russia)

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We have synthesized and characterized a panel of new binuclear mixed valence Cu(I,II) complexes containing substituted 2-alkylthio-5-arylmethylene-4H-imidazolin-4-ones with unusual structure. These complexes are shown to be cytotoxic for various cell lines. We have found that these compounds did not intercalate DNA, inhibited number of polymerases (telomerase predominantly), accumulated in the cell nucleus, and caused DNA degradation. Preliminary studies revealed that lead compound inhibited human breast adenocarcinoma growth in mice model.

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