Metal complexes are important chemotherapeutic agents against diseases; cisplatin is a widely used antitumor agent. Other metal centers are promising and ruthenium complexes are already in pre-clinical trials. Recently, we described the excellent antitumor activity on colon-rectal tumor cell line of a ruthenium-curcumin complex and we described the interaction of this complex with the metal binding to guanine N7 of a DNA moiety (Caruso F, Rossi M, Benson A, Opazo C, Freedman D, Monti E, Gariboldi MB, Shaulky J, Marchetti F, Pettinari R, Pettinari C. J Med Chem. 2012 55, 1072). We present here a novel series of Ru compounds where curcumin is replaced with several beta-diketone ligands. One has particularly strong antitumor activity in vitro; in observing the structure-activity relationship, we hypothesize a potential intercalation of the ligand naphthalene moiety in between the bases of DNA. We describe a theoretical docking procedure for this species and also include antitumor activity and X-ray diffraction studies.
A novel series of antitumor ruthenium beta-diketonato compounds
PETTINARI, Claudio;MARCHETTI, Fabio;PETTINARI, Riccardo;
2013-01-01
Abstract
Metal complexes are important chemotherapeutic agents against diseases; cisplatin is a widely used antitumor agent. Other metal centers are promising and ruthenium complexes are already in pre-clinical trials. Recently, we described the excellent antitumor activity on colon-rectal tumor cell line of a ruthenium-curcumin complex and we described the interaction of this complex with the metal binding to guanine N7 of a DNA moiety (Caruso F, Rossi M, Benson A, Opazo C, Freedman D, Monti E, Gariboldi MB, Shaulky J, Marchetti F, Pettinari R, Pettinari C. J Med Chem. 2012 55, 1072). We present here a novel series of Ru compounds where curcumin is replaced with several beta-diketone ligands. One has particularly strong antitumor activity in vitro; in observing the structure-activity relationship, we hypothesize a potential intercalation of the ligand naphthalene moiety in between the bases of DNA. We describe a theoretical docking procedure for this species and also include antitumor activity and X-ray diffraction studies.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
