Pt(IV) anticancer compounds typically operate as prodrugs that are reduced in the hypoxic environment of cancer cells, losing two axial ligands in the process to generate active Pt(II) species. Here we report the synthesis of two fluorescent Pt(IV) prodrugs of cisplatin in order to image and evaluate the Pt(IV) reduction process in simulated and real biological environments. Treatment of the co...

A platinum(II) and 3 platinum! l\ i ammine/cycloalkylamine ho mologous series were evaluated for cytotoxicity and biochemical pharmacology in murine leukemia L1210/0, cis-diamminedichloroplatinum(H)-resistant 1.1210/1)1)1', and diaminocyclohexaneplatinum-resistant L1210/l,2-diaminocyclohexane (DACH) cells. Within each se ries, which contained 4 homologues with differing alicyclic (cycloalkyl) r...

A straightforward, one-pot procedure has been developed for the synthesis of bis-cyclometalated chloro(methyl)platinum(IV) complexes with a wide variety of heteroaromatic ligands of the 2-arylpyridine type. The new compounds exhibit phosphorescent emissions in the blue to orange colour range and represent the most efficient Pt(IV) emitters reported to date, with quantum yields up to 0.81 in flu...

Platinum compounds represent one of the great success stories of metals in medicine. Following the serendipitous discovery of the anticancer activity of cisplatin by Rosenberg, a large number of cisplatin variants have been prepared and tested for their ability to kill cancer cells and inhibit tumor growth. These efforts continue today with increased realization that new strategies are needed t...

A series of stable platinum complexes containing closo-carborane cages in a 'carrier group', which could be potentially utilized for boron neutron capture therapy (BNCT), was successfully synthesized and characterized by various spectroscopic methods. Two ortho-closo-carborane cages were connected to the 3,3' or 4,4'-positions of 2,2'-bipyridine through ester bonds to give three carborane-linke...

We report two platinum(IV) complexes conjugated with a vitamin E analog, α-tocopherol succinate (α-TOS). One of the conjugates displays the activity of both cisplatin and α-TOS in cancer cells, causing damage to DNA and mitochondria simultaneously. Accordingly, it serves as a promising dual-targeting anticancer agent.