Ruthenium (II) nitrofurylsemicarbazone complexes: new DNA binding agents.
Complexes of the type [Ru(II)Cl(2)(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to combine the potential anti-tumor activity of the metal and the free ligands. The new complexes are excellent DNA binding agents for calf thymus DNA. So, their in vitro anti-tumor activity was tested in cellular models and the complexes were found to be non-cytotoxic on the tumor cell lines assayed, neither in aerobic conditions nor in the bio-reductive assay performed. Redox behavior, lipophilicity and stability were studied in order to explain the lack of cellular cytotoxic effects. The complexes resulted 10-100 times more hydrophilic than the parent ligands thus the bio-activity of these compounds would be compromised by their inadequate lipophilic properties.
Cabrera
Eliana
E
Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
Cerecetto
Hugo
H
González
Mercedes
M
Gambino
Dinorah
D
Noblia
Pabla
P
Otero
Lucía
L
Parajón-Costa
Beatriz
B
Anzellotti
Atilio
A
Sánchez-Delgado
Roberto
R
Azqueta
Amaia
A
López de Ceráin
Adela
A
Monge
Antonio
A
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D018736:DNA Adducts / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D009593:Nitroimidazoles / Q000737:chemistry; D009942:Organometallic Compounds / Q000737:chemistry / Q000494:pharmacology; D010084:Oxidation-Reduction; D012428:Ruthenium / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D018736:DNA Adducts; D009593:Nitroimidazoles; D009942:Organometallic Compounds; D012428:Ruthenium; D004247:DNA; C427203:calf thymus DNA