Arene-ruthenium(II) acylpyrazolonato complexes: Apoptosis-promoting effects on human cancer cells

R. Pettinari, C. Pettinari, F. Marchetti, Brian Skelton, Allan White, L. Bonfili, M. Cuccioloni, M. Mozzicafreddo, V. Cecarini, M. Angeletti, M. Nabissi, A.M. Eleuteri

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79 Citations (Scopus)


A series of ruthenium(II) arene complexes with the 4-(biphenyl-4-carbonyl)- 3-methyl-1-phenyl-5-pyrazolonate ligand, and related 1,3,5-triaza-7- phosphaadamantane (PTA) derivatives, has been synthesized. The compounds have been characterized by NMR and IR spectroscopy, ESI mass spectrometry, elemental analysis, and X-ray crystallography. Antiproliferative activity in four human cancer cell lines was determined by MTT assay, yielding dose- and cancer cell line-dependent IC50 values of 9-34 μM for three hexamethylbenzene-ruthenium complexes, whereas the other metal complexes were much less active. Apoptosis was the mechanism involved in the anticancer activity of such compounds. In fact, the hexamethylbenzene-ruthenium complexes activated caspase activity, with consequent DNA fragmentation, accumulation of pro-apoptotic proteins (p27, p53, p89 PARP fragments), and the concomitant down-regulation of antiapoptotic protein Bcl-2. Biosensor-based binding studies indicated that the ancillary ligands were critical in determining the DNA binding affinities, and competition binding experiments further characterized the nature of the interaction. © 2014 American Chemical Society.
Original languageEnglish
Pages (from-to)4532-4542
JournalJournal of Medicinal Chemistry
Issue number11
Publication statusPublished - 2014


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