title: PdIIand PtIIcomplexes with a thio-aza macrocycle ligand containing an intercalating fragment: Structural and antitumor activity studies.
abstract: Two new PtIIand PdIIcomplexes of formula [LMCl2] (M=Pt, Pd) were synthesized and characterized both in solution and solid state. They were obtained using the thio-aza macrocycle 9,18-dimethyl-12,17dithia-9,18,27,28-tetraaaza-29-oxatetracyclo[24.2.1.02,7.020,25]enneicosa-2,4,6,20,22,24,26,281-octaene (L) containing the 2,5-diphenyl [1, 3, 4]oxadiazole as intercalating fragment. MIIis coordinated in cis-position by the two S atoms of L. The two crystal structures of [LPtCl2] and [LPdCl2] complexes showed that the MIIion is located outside the macrocyclic cavity. The square planar coordination sphere is fulfilled by two chloride anions in a cisplatin-like arrangement with the chloride leaving groups exposed to the environment. The biological activity of both [LPtCl2] and [LPdCl2], monitored towards a leukemic cellular model (U937), is coherent with their ability to interfere, at different levels, with the DNA structure.
authors.affiliation: University of Urbino, Molecular Pathology Lab. "PaoLa", Department of Biomolecular Sciences, Arco d'Augusto 2, I-61032 Fano, (PU), Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Amatori
authors.affiliation: University of Urbino, Department of Pure and Applied Sciences, Via della Stazione 4, I-61029 Urbino, Italy.
authors.forename: Gianluca
authors.initials: G
authors.lastname: Ambrosi
authors.affiliation: University of Urbino, Molecular Pathology Lab. "PaoLa", Department of Biomolecular Sciences, Arco d'Augusto 2, I-61032 Fano, (PU), Italy.
authors.forename: Alfredo
authors.initials: A
authors.lastname: Errico Provenzano
authors.affiliation: University of Urbino, Molecular Pathology Lab. "PaoLa", Department of Biomolecular Sciences, Arco d'Augusto 2, I-61032 Fano, (PU), Italy. Electronic address: mirco.fanelli@uniurb.it.
authors.forename: Mirco
authors.initials: M
authors.lastname: Fanelli
authors.affiliation: University of Urbino, Department of Pure and Applied Sciences, Via della Stazione 4, I-61029 Urbino, Italy.
authors.forename: Mauro
authors.initials: M
authors.lastname: Formica
authors.affiliation: University of Urbino, Department of Pure and Applied Sciences, Via della Stazione 4, I-61029 Urbino, Italy. Electronic address: vieri.fusi@uniurb.it.
authors.forename: Vieri
authors.initials: V
authors.lastname: Fusi
authors.affiliation: University of Urbino, Department of Pure and Applied Sciences, Via della Stazione 4, I-61029 Urbino, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Giorgi
authors.affiliation: University of Firenze, Department of Industrial Engineering, Via S. Marta 3, I-50139 Firenze, Italy.
authors.forename: Eleonora
authors.initials: E
authors.lastname: Macedi
authors.affiliation: University of Urbino, Department of Pure and Applied Sciences, Via della Stazione 4, I-61029 Urbino, Italy.
authors.forename: Mauro
authors.initials: M
authors.lastname: Micheloni
authors.affiliation: University of Firenze, Department of Industrial Engineering, Via S. Marta 3, I-50139 Firenze, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Paoli
authors.affiliation: University of Firenze, Department of Industrial Engineering, Via S. Marta 3, I-50139 Firenze, Italy.
authors.forename: Patrizia
authors.initials: P
authors.lastname: Rossi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001372:Aza Compounds / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000494:pharmacology; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008024:Ligands; D015394:Molecular Structure; D009000:Monocytes / Q000187:drug effects / Q000473:pathology; D010165:Palladium / Q000737:chemistry*; D010957:Plasmids / Q000737:chemistry; D010984:Platinum / Q000737:chemistry*; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D056831:Coordination Complexes; D007364:Intercalating Agents; D008024:Ligands; D013844:Thiazoles; D010984:Platinum; D010165:Palladium; D004247:DNA; D002945:Cisplatin
keywords: Antineoplastic drugs; Cancer; Macrocycle; Palladium complexes; Platinum complexes