Albumin-targeting of a maleimide-containing oxaliplatin-releasing platinum(iv) prodrug results in tumor-specific drug delivery and activity as shown by LA-ICP-MS, isotope-labeling and NanoSIMS in cell culture and in vivo.

The reductive biotransformation of platinum(iv) prodrugs was investigated in whole human blood by HPLC-ICP-MS.

An unsymmetrically carboxylated platinum(IV) analogue of oxaliplatin was coupled to low-generation polyamidoamine dendrimers (PAMAM) with amino-terminated surfaces [generations two (G-2) and four (G-4)]. 1D and 2D diffusion NMR spectroscopy and high-resolution HPLC-MS/MS were used to characterise the platinum complexes and drug-dendrimer conjugates. The average loads of platinum(IV) complex per dendrimer were determined by inductively coupled plasma MS (ICP-MS), and maximum loads of 38 % (six platinum units per dendrimer molecule) for the smaller G-2 and 34 % (22 platinum units per dendrimer molecule) for G-4 were obtained. As a result of this loading, the average diameters increased from 26 to 34 Å (30 %, G-2) and from 46 to 63 Å (38 %, G-4). The in vitro

Three copper(II) complexes of a series of bidentate dipyridylmethane ligands, as well as their structurally related platinum(II) analogues, have been synthesised and fully characterised to evaluate their coordination chemistry and antiproliferative properties. New crystal structures of the complexes L3CuCl2, L2PtCl2 and L3PtCl2, where L2, L3 have one and two methyl substituents on the bridgehead carbon atom between the coordinated pyridine ligands, respectively, were obtained. The in vitro cytotoxicity of the free ligands and their corresponding platinum and copper complexes was evaluated in the cisplatin‐sensitive ovarian teratocarcinoma cell line CH1/PA1, as well as in rather cisplatin‐insensitive colon (SW480) and lung (A549) carcinoma cells, using the MTT assay. All six complexes showed higher cytotoxicity than the ligands L1–L3 alone, giving IC50 values in the low micromolar range.

Oxaliplatin shows a superior clinical activity in colorectal cancer compared to cisplatin. Nevertheless, the knowledge about its cellular distribution and the mechanisms responsible for the different range of oxaliplatin-responsive tumors...