title: Highly cytotoxic DNA-interacting copper(II) coordination compounds.
abstract: Four new Schiff-base ligands have been designed and prepared by condensation reaction between hydrazine derivatives (i.e. 2-hydrazinopyridine or 2-hydrazinoquinoline) and mono- or dialdehyde (3-tert-butyl-2-hydroxybenzaldehyde and 5-tert-butyl-2-hydroxyisophthalaldehyde, respectively). Six copper(II) coordination compounds of various nuclearities have been obtained from these ligands, which are formulated as [Cu(L1)Cl](CH3OH) (1), [Cu(L2)NO3] (2), [Cu2(L3)(ClO4)2(CH3O)(CH3OH)](CH3OH) (3), [Cu2(L4)(ClO4)(OH)(CH3OH)](ClO4) (4), [Cu8(L3)4(NO3)4(OH)5](NO3)3(CH3OH)5(H2O)8 (5) and [Cu3(HL2')4Cl6](CH3OH)6 (6), as revealed by single-crystal X-ray studies. Their DNA-interacting abilities have been investigated using different characterization techniques, which suggest that the metal complexes act as efficient DNA binders. Moreover, cytotoxicity assays with several cancer cell lines show that some of them are very active, as evidenced by the sub-micromolar IC50 values achieved in some cases.
authors.affiliation: Departament de Química Inorgànica, Universitat de Barcelona, Martí i Franquès 1-11, 08028 Barcelona, Spain. patrick.gamez@qi.ub.es.
authors.forename: Rosa F
authors.initials: RF
authors.lastname: Brissos
authors.forename: Ester
authors.initials: E
authors.lastname: Torrents
authors.forename: Francyelli Mariana
authors.initials: FM
authors.lastname: dos Santos Mello
authors.forename: Wanessa
authors.initials: W
authors.lastname: Carvalho Pires
authors.forename: Elisângela de Paula
authors.initials: Ede P
authors.lastname: Silveira-Lacerda
authors.forename: Ana B
authors.initials: AB
authors.lastname: Caballero
authors.forename: Amparo
authors.initials: A
authors.lastname: Caubet
authors.forename: Chiara
authors.initials: C
authors.lastname: Massera
authors.forename: Olivier
authors.initials: O
authors.lastname: Roubeau
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Teat
authors.forename: Patrick
authors.initials: P
authors.lastname: Gamez
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D003300:Copper / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D006801:Humans; D006834:Hydrazines / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D003603:Cytotoxins; D006834:Hydrazines; D003300:Copper; D004247:DNA