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Cyclometalated Iminophosphorane Gold(III) and Platinum(II) Complexes. A Highly Permeable Cationic Platinum(II) Compound With Promising Anticancer Properties

Cyclometalated Iminophosphorane Gold(III) and Platinum(II) Complexes. A Highly Permeable Cationic Platinum(II) Compound With Promising Anticancer Properties

Malgorzata Frik, Jacob Fernández-Gallardo, Oscar Gonzalo, Víctor Mangas-Sanjuan, Marta González-Alvarez, Alfonso Serrano del Valle, Chunhua Hu, Isabel González-Alvarez, Marival Bermejo, Isabel Marzo, María Contel

J Med Chem. 2015 Aug 13;58(15):5825-41.

PMID: 26147404

Abstract:

New organometallic gold(III) and platinum(II) complexes containing iminophosphorane ligands are described. Most of them are more cytotoxic to a number of human cancer cell lines than cisplatin. Cationic Pt(II) derivatives 4 and 5, which differ only in the anion, Hg2Cl6(2-) or PF6(-) respectively, display almost identical IC50 values in the sub-micromolar range (25-335-fold more active than cisplatin on these cell lines). The gold compounds induced mainly caspase-independent cell death, as previously reported for related cycloaurated compounds containing IM ligands. Cycloplatinated compounds 3, 4, and 5 can also activate alternative caspase-independent mechanisms of death. However, at short incubation times cell death seems to be mainly caspase dependent, suggesting that the main mechanism of cell death for these compounds is apoptosis. Mercury-free compound 5 does not interact with plasmid (pBR322) DNA or with calf thymus DNA. Permeability studies of 5 by two different assays, in vitro Caco-2 monolayers and a rat perfusion model, have revealed a high permeability profile for this compound (comparable to that of metoprolol or caffeine) and an estimated oral fraction absorbed of 100%, which potentially makes it a good candidate for oral administration.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP109632088	Metoprolol Related Compound A		109632-08-8	Price

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