The discovery of cisplatin (cis-Pt(NH3)2Cl2) as an antineoplastic agent has focused attention on the rational design of metal complexes that can be potentially used in cancer chemotherapy. Today, the pharmaceutical industry invests more than $1 billion each year in the development of new metal-based drugs to improve biological activities, in terms of cellular selectivity, therapeutic efficiency and minimization of side effects. Chemotherapies based on transition metals play a key role in cancer treatment, and among them platinum and palladium are the most fruitful. This article reviews the main recent advances in the design and synthesis of platinum- and palladium-based drugs, their structural features and biological studies of them. The rationale for the choice of the ligand, related to leaving groups, the geometry of the complex and the oxidation state of the metal ion, is discussed. An overview of the main biological techniques and approaches for testing the interaction of these molecules with the biological environment, mainly DNA, to validate the effect is also provided.

New trends in platinum and palladium complexes as antineoplastic agents

FANELLI, MIRCO;FORMICA, MAURO;FUSI, VIERI
;
GIORGI, LUCA;MICHELONI, MAURO SERGIO
;
2016

Abstract

The discovery of cisplatin (cis-Pt(NH3)2Cl2) as an antineoplastic agent has focused attention on the rational design of metal complexes that can be potentially used in cancer chemotherapy. Today, the pharmaceutical industry invests more than $1 billion each year in the development of new metal-based drugs to improve biological activities, in terms of cellular selectivity, therapeutic efficiency and minimization of side effects. Chemotherapies based on transition metals play a key role in cancer treatment, and among them platinum and palladium are the most fruitful. This article reviews the main recent advances in the design and synthesis of platinum- and palladium-based drugs, their structural features and biological studies of them. The rationale for the choice of the ligand, related to leaving groups, the geometry of the complex and the oxidation state of the metal ion, is discussed. An overview of the main biological techniques and approaches for testing the interaction of these molecules with the biological environment, mainly DNA, to validate the effect is also provided.
File in questo prodotto:
File Dimensione Formato  
N126_CCR1_16.pdf

non disponibili

Descrizione: Articolo
Tipologia: Versione editoriale
Licenza: Pubblico con Copyright
Dimensione 3.68 MB
Formato Adobe PDF
3.68 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Revised manuscript CoorChemRev2016.pdf

accesso aperto

Tipologia: Versione referata/accettata
Licenza: Creative commons
Dimensione 904.9 kB
Formato Adobe PDF
904.9 kB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11576/2629485
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 200
  • ???jsp.display-item.citation.isi??? 197
social impact