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. Supported by HHMI52006322.
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