2. Academic Validation
  3. Cyclopalladated primary amines: a preliminary study of antiproliferative activity through apoptosis induction

Cyclopalladated primary amines: a preliminary study of antiproliferative activity through apoptosis induction

  • Eur J Med Chem. 2014 Sep 12:84:530-6. doi: 10.1016/j.ejmech.2014.07.046.
Joan Albert 1,  Ramon Bosque 2,  Margarita Crespo 2,  Graciela García 3,  Jaume Granell 2,  Concepción López 4,  María Victoria Lovelle 3,  Romana Qadir 3,  Asensio González 5,  Anusha Jayaraman 6,  Enric Mila 6,  Roldán Cortés 6,  Josefina Quirante 5,  Carme Calvis 7,  Ramon Messeguer 7,  Josefa Badía 8,  Laura Baldomà 8,  Marta Cascante 9
Affiliations

Affiliations

  • 1 Departament de Química Inorgànica, Facultat de Química, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain; Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain. Electronic address: [email protected].
  • 2 Departament de Química Inorgànica, Facultat de Química, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain; Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain.
  • 3 Departament de Química Inorgànica, Facultat de Química, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain.
  • 4 Departament de Química Inorgànica, Facultat de Química, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain. Electronic address: [email protected].
  • 5 Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain; Laboratori de Química Orgànica, Facultat de Farmàcia, Universitat de Barcelona, Av. Joan XXIII, s/n, 08028 Barcelona, Spain.
  • 6 Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain; Department of Biochemistry and Molecular Biology, Faculty of Biology, Universitat de Barcelona, Unit Associated with CSIC, Diagonal 643, 08028 Barcelona, Spain.
  • 7 Biomed Division LEITAT Technological Center, Parc Científic, Edifici Hèlix, C/ Baldiri Reixach, 15-21, 08028 Barcelona, Spain.
  • 8 Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain; Departament de Bioquímica i Biologia Molecular, Facultat de Farmàcia, Universitat de Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain.
  • 9 Institut de Biomedicina (IBUB), Universitat de Barcelona, Barcelona, Spain; Department of Biochemistry and Molecular Biology, Faculty of Biology, Universitat de Barcelona, Unit Associated with CSIC, Diagonal 643, 08028 Barcelona, Spain; Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), Spain.
PMID: 25063943 DOI: 10.1016/j.ejmech.2014.07.046
Abstract

Twelve cyclometallated palladium(II) complexes containing primary aromatic amines [benzylamine (a), (R)-1-(1-naphthyl)ethylamine (b) and 2-phenylaniline (c)] as anionic bidentate (C,N)(-) ligands have been evaluated against a panel of human adenocarcinoma cell lines (A549 lung, MDA-MB231 and MCF7 breast, and the cisplatin resistant HCT116 colon). The results revealed a remarkable antiproliferative activity of the triphenylphosphane mononuclear compounds 3-4 (series a, b, c) and the best inhibition was provided for 3c and 4c with the 2-phenylaniline ligand and a six membered chelate ring. Interestingly, 3c and 4c were 14 and 19 times more potent than cisplatin for the inhibition of the cisplatin resistant HCT116 human adenocarcinoma cell line, respectively. Cyclopalladated complexes 3c and 4c exercise their antiproliferative activity over A549 cells mainly through the induction of Apoptosis (38 and 31-fold increase in early apoptotic cells, respectively).

Keywords

Anticancer drugs; Cyclopalladated complexes; Cytotoxicity; Palladium(II).

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