The alkyne functionalised bidentate N-donor ligand (2-propargyloxyphenyl)bis(pyrazolyl)methane was prepared in high yield from the reaction of (2-hydroxyphenyl)bis(pyrazolyl)methane with propargyl bromide in the presence of base. A series of transition-metal complexes including [MCl2] (M=Cu, Co, Ni, Zn, Pt), [M2](NO3)2 (M=Cu, Co, Ni, Zn), [Ag]NO3 and [Pd(dppe)](OTf)2 were prepared and character...

Mixed amine/ammine motifs are important features in newer generation platinum anticancer agents, including the Pt(IV) prodrug satraplatin. One synthetic route that can be used to access platinum molecules with such structures exploits the trans effect during NH3-mediated cleavage of iodo-bridged platinum(II) dimers of the form [Pt(Am)I(μ-I)]2, where Am is an amine. A clear picture of the nature...

A microwave-assisted synthesis of cisplatin, cis-[Pt(NH3)2Cl2], has been developed and optimized on both a 0.2 and 0.05 millimolar scale. The optimized synthetic procedure was modeled after the Lebedinskii-Golovnya method and is suitable for incorporating the radionuclide, (195m)Pt, into cisplatin for biological studies. Highest yields (47%) and purity are obtained using a K2PtCl4 : NH4OAc : KC...

Periana et al. [Science 1998, 280, 560] previously reported two catalysts for lowtemperature methane activation to methanol: PtCl2(NH3)2 and PtCl2(bpym). It was shown that the ammine catalyst is much more active, but it decomposes rapidly in sulfuric acid to form a PtCl2 precipitate, while the bpym system is long-lived. To have a basis for developing new catalysts that would not decompose, we u...

Cisplatin (cis-diamminedichloroplatinum II, cisPt) is especially useful in the treatment of epithelial malignancies, however, the use of cisplatin is accompanied by several toxicities including haematological toxicity. Contrary to cisplatin, selenium-cisplatin conjugate ((NH(3))(2)Pt(SeO(3)); Se-Pt) has only a slight toxicity effect on blood platelet function. In the mechanism of platinum compo...

In an effort to expand the therapeutic range of platinum anticancer agents, several new approaches to platinum-based therapy, including nanodelivery, are under active investigation. To better understand the effect of ligand lipophilicity on the encapsulation of Pt(IV) prodrugs within polymer nanoparticles, the series of compounds cis,cis,trans-[Pt(NH3)2Cl2L2] was prepared, where L = acetate, pr...

The synthesis and characterization of a series of picoplatin-based (picoplatin = [PtCl(2)(mpy)(NH(3))], mpy = 2-methylpyridine), Pt(iv) complexes with axial carboxylato ligands of increasing length are reported. The synthesis is based on the oxidation with hydrogen peroxide of picoplatin to give the cis,cis,trans-[PtCl(2)(mpy)(NH(3))(OH)(2)] intermediate and then its transformation into the dic...

In the mol-ecular structure of the dinuclear title compound [η(5)-(C5(CH3)5)(CO)Fe{(μ-BCl)(μ-CO)}PtCl(P(C6H11)3)]·C6H6, the two metal atoms, iron(II) and platinum(II), are bridged by one carbonyl (μ-CO) and one chlorido-borylene ligand (μ-BCl). The Pt(II) atom is additionally bound to a chloride ligand situated trans to the bridging borylene, and a tri-cyclo-hexyl-phosphane ligand (PCy3) trans ...

Our aim was to determine whether a single transplatin monofunctional adduct, either trans-[Pt(NH3)2(dC)Cl]+ or trans-[Pt(NH3)2(dG)Cl]+ within a homopyrimidine oligonucleotide, could further react and form an interstrand cross-link once the platinated oligonucleotide was bound to the complementary duplex. The single monofunctional adduct was located at either the 5' end or in the middle of the p...

Reports on toxic effects of platinum coordination complexes on the endocrine pancreas are missing with exception of cis-DDP itself (Goldstein et al 1983). Recently, oxoplatin (trans-dihydroxy-cis-dichlorodiammine-platinum [IV]) an oxygenated derivative of cis-DDP has been described by Presnov and Konovalova (1988), Fig. 1. As indicated by the maximally tolerated dose levels, oxoplatin has been ...