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

Eur J Med Chem

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.

Published: September 2014

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).

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http://dx.doi.org/10.1016/j.ejmech.2014.07.046DOI Listing

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