Design and biological evaluation of new platinum(II) complexes bearing ligands with DNA-targeting ability.
A novel series of platinum(II) complexes bearing aliphatic amines and ligands with DNA-targeting properties was synthesized to achieve more potent and selective metallodrugs. We developed six new platinum-based drugs, which contain methylamine, 1a-c, and isopropylamine, 2a-c, both in the trans position to a selected targeting ligand: naphthalimide. The activity of the complexes has been evaluated in order to confirm the improvements from our proposed approach, and the complexes demonstrate better cytotoxic activity on cancer cell lines when compared with the ligands and, importantly, with cisplatin. Further studies were performed to assess their subcellular localization and binding mode to DNA.
Departamento de Química Inorgánica, Facultad de Ciencias, Universidad Autónoma de Madrid , Francisco Tomás y Valiente 7, 28049 Madrid, Spain.
Jacqueline M
JM
Herrera
Filipa
F
Mendes
Sofia
S
Gama
Isabel
I
Santos
Carmen
C
Navarro Ranninger
Silvia
S
Cabrera
Adoración G
AG
Quiroga
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D017671:Platinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013054:Spectrophotometry, Atomic
D000970:Antineoplastic Agents; D008024:Ligands; D017671:Platinum Compounds; D004247:DNA