Metal complexes as structural templates for targeting proteins

Metal complexes as “protein surface mimetics”

“…2), thus expanding the number of globular shapes available and allowing exploration of protein pockets and surfaces inaccessible to conventional small organic molecules. 23 Metal complexes also have the ability to exist in many more stereoisomers than organic molecules, for example an sp 3 carbon with 4 different substituents has only two possible stereoisomers whereas an octahedral metal centre with 6 different ligands can exist in up to 30 different stereoisomers (Fig. 2).…”

Selective cytotoxicity of arene tricarbonylchromium towards tumour cell lines

“…Organometallic compounds have been extensively studied for their applications in medicine over the last two decades [13][14][15][16][17][18]. The first fruit was arsphenamine (Salvarsan), which is based on arsenic (despite its unfavourable reputation as poison) and azobenzene, serving for the treatment of syphilis and trypanosomiasis.…”

Osmocenyl-tamoxifen derivatives target the thioredoxin system leading to a redox imbalance in Jurkat cells

“…To that can be added the variety of available metals [2] and, for the transition elements, the potential availability of several degrees of oxidation. 3 With organometallic complexes of gold [8,9], those from the group 8 triad, particularly of Fe and Ru, are amongst the most widely studied [10][11][12][13] with the notable exception to date of Os [14][15][16][17]. This heavy element offers a capacity for good stabilization of certain high degrees of oxidation (+VI) and for an excellent metal-to-ligand back-donation at low oxidation states (+II, +III) leading to more stable complexes than those of Fe or Ru in biological media.…”

“…For this reason, the unusual mechanistic properties of organometallic medicinal chemistry are presently the subject of an exponentially growing number of studies [1]. These entities offer inventive strategic approaches [2][3][4][5][6] in terms of optimized space filling, intracellular redox behavior and antitumoral activity, with pharmacophores possessing varied and multiple targeting options that make it possible to counteract the phenomena of resistance to proapoptotic stimuli [7]. To that can be added the variety of available metals [2] and, for the transition elements, the potential availability of several degrees of oxidation.…”