The anti-arthritic drug auranofin exerts also potent antitumour activity in in vitro and in vivo models, whose mechanisms are not yet well defined. From an auranofin-sensitive human ovarian cancer cell line A2780, a highly resistant (>20-fold) subline (A2780/AF-R) was developed and characterized. Marked reduction of gold accumulation occurred in auranofin-resistant A2780 cells. Also, moderately...

This review is aimed at providing a concise overview of the results obtained by our group in field organometallic chemistry gold. Therefore, selection examples amongst most extensively explored families bioactive gold complexes — Au(I) N-heterocyclic carbenes and cyclometalated Au(III) compounds presented. Insights into bio-inorganic mechanisms reactivity organogold an integrated investigationa...

A relatively rare form of arthritis was described by Hench and Rosenberg in 1941 and in 1944. The syndrome is characterized by frequently recurring attacks of pain, swelling, redness, and disability involving usually one joint at a time, but sometimes multiple joints. The attacks last for short periods and then subside completely without leaving -joint residue. They considered it to be a " new ...

The chemical reactivity of Au(I)compounds is related to their HOMO-LUMO energy separation. For coordinately unsaturated complexes of Au(I), the excited state (HOMO-LU_MO separation) is only about 2 eV above the ground state. Many Au(I)complexes such as [Au(TPPTS)3]8-and [Au(TPA)3] show visible luminescence from this state even in water solution. Quenching of the phosphorescence relates to the r...

Gold(III) complexes are emerging as a new class of metal complexes with outstanding cytotoxic properties and are presently being evaluated as potential antitumor agents. This renewed interest is the result of recent studies in which various gold(III) complexes have been shown to be stable under physiological conditions and to manifest relevant antiproliferative properties against selected human...

Cancer is an umbrella term used to describe a variety of diseases in which cells start dividing abnormally. These cells then spread through blood and lymph system to invade other tissues of the body. There exist more than 100 different types of cancer. Depending upon the site of origin, cancer can be grouped as carcinoma (starting in the skin or tissue lining of internal organs), sarcoma (cance...

The reaction of N,N'-bis(2,6-diisopropylphenyl)imidazol-2-ylidene gold hydroxide ([Au(OH)(IPr)]; 1) with acetylene and trimethylsilylacetylene derivatives cleanly leads to the formation of a gold-acetylide bond with the concomitant formation of water or trimethylsilanol. All compounds were isolated in high yield (>85%). The crystal structures of selected gold acetylides in conjunction with thei...

The recent development of new gold(I) catalysis methodologies has opened the door to new disconnections for the total synthesis of bioactive complex molecules. Below is described the application of a gold(I)-catalyzed hydroarylation of an allene with indole toward the total synthesis of flinderoles B-C, members of a new class of antimalarial bisindole alkaloids isolated from plants of the Flind...

A class of phosphane gold(I) compounds, made azoles and ligands, was evaluated for a screening on the regards Breast Cancer cell panels (BC). The compounds possess N-Au-P or Cl-Au-P bonds around central metal, they differ presence aprotic protic polar groups in and/or moieties to tune their hydrophilicity. Among six candidates, only having P-Au-N environment not displaying neither hydroxyl nor ...

To the Editor: In their interesting paper, Sfikakis et a1 state " no previous study, to our knowledge, has investigated the in vitro effects of gold compounds on the IL-2/IL-2R [interleukin-2/interleukin-2 receptor] system " (1). This is an oversight, since my colleagues and I have previously shown an in vitro effect of gold sodium thiomalate (GST) on the IL-2/IL-2R system (2). In our experimen...