The discovery of cisplatin (cis-Pt(NH3)2Cl2) as an antineoplastic agent has focussed attention on therational design of metal complexes that can be potentially used in cancer chemotherapy. Today, thepharmaceutical industry invests more than $1 billion each year in the development of new metal-baseddrugs to improve biological activities, in terms of cellular selectivity, therapeutic efficiency and mini-mization 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 recentadvances in the design and synthesis of platinum- and palladium-based drugs, their structural featuresand biological studies of them. The rationale for the choice of the ligand, related to leaving groups, thegeometry of the complex and the oxidation state of the metal ion, is discussed. An overview of the mainbiological techniques and approaches for testing the interaction of these molecules with the biologicalenvironment, 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; Paoli, Paola. - In: COORDINATION CHEMISTRY REVIEWS. - ISSN 0010-8545. - ELETTRONICO. - 310:(2016), pp. 41-79. [10.1016/j.ccr.2015.11.004]
New trends in platinum and palladium complexes as antineoplastic agents
PAOLI, PAOLA
2016
Abstract
The discovery of cisplatin (cis-Pt(NH3)2Cl2) as an antineoplastic agent has focussed attention on therational design of metal complexes that can be potentially used in cancer chemotherapy. Today, thepharmaceutical industry invests more than $1 billion each year in the development of new metal-baseddrugs to improve biological activities, in terms of cellular selectivity, therapeutic efficiency and mini-mization 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 recentadvances in the design and synthesis of platinum- and palladium-based drugs, their structural featuresand biological studies of them. The rationale for the choice of the ligand, related to leaving groups, thegeometry of the complex and the oxidation state of the metal ion, is discussed. An overview of the mainbiological techniques and approaches for testing the interaction of these molecules with the biologicalenvironment, mainly DNA, to validate the effect is also provided.File | Dimensione | Formato | |
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