Complessi ditiocarbammici di oro (III) eloro impiego come antitumorali - Dithiocarbamate complexes of gold(III) and their use as antitumor agents

L’invenzione è relativa a complessi quadrato-planari ditiocabammici di oro(III), al loro processo di sintesi ed al loro impiego terapeutico per il trattamento di patologie tumorali. I complessi di oro(III) dell’invenzione hanno infatti dimostrato di avere un vantaggioso effetto farmacologico in quanto più efficaci rispetto al cis-platino. Inoltre tali complessi dell’oro(III) risultano non presentare né fenomeni di resistenza crociata né di tossicità tipici del cis-platino. - The synthesis of claimed planar square gold(III) dithiocarbamic complexes for use as antitumor agents is described. The compds. with substituted dithiocarbamate and 2 halogen (Cl, Br) ligands are defined by Markush structures. Several complex compds. were synthesized by std. procedures and the products were characterized by IR, 1H-NMR and 13C-NMR spectroscopy, elemental anal., m.p., soly., and elec. cond. The compds. were tested for toxicity and antitumor activity in vitro using human tumor cell lines and in mice with transplanted solid and liq. tumors. The gold complexes had antitumor activities comparable with the effects of cisplatin, but showed less cross-resistance development and less toxicity compared to cisplatin. The gold complexes can be formulated with std. pharmaceutical excipients into forms suitable for oral treatment use (emulsions, suspensions, powders, gelatin capsules, tablets). The formulations can be also used for topical and transdermal treatments and for purging tumor cells from bone marrow autotransplants.