Abstract
New dithiocarbamate cycloaurated complexes have been synthesized and their physicochemical and in vitro antitumor properties have been evaluated. All the performed studies highlighted good transport through the blood and biodistribution, according to the balance between the properties of hydrophilicity/lipophilicity and the binding of moderate strength to the BSA protein. Furthermore, none of the complexes exhibited reduction or decomposition reactions, presenting excellent physiological stability. The in vitro cytotoxic effect was evaluated on human colon cancer cell line Caco-2/TC7, and the complexes showed great antiproliferative activity and excellent selectivity, as much less effect was detected on normal Caco-2/TC7 cells. Most of the complexes exhibit antiproliferative activity that was better than or similar to auranofin, and at least nine times better than that of cisplatin. Its action mechanism is still under discussion since no evidence of cell cycle arrest was found, but an antioxidant role was shown for some of the selective complexes. All complexes were also tested as antimicrobial drugs, exhibiting good activity towards S. aureus and E. coli. bacteria and C. albicans and C. neoformans fungi.
Highlights
IntroductionPlatinum-based anticancer drugs have been developed during this time, and four platinum(II) drugs are approved for use in chemotherapy [4], cisplatin continues to be the most widely used together with the second-generation drug carboplatin [Pt(NH3 ) (CBDCA-O,O0 )]
The dithiocarbamate derivatives were obtained by a one-pot reaction of the parent dichloro complex with the selected sodium salt of the DTC ligand
We report on the synthesis of new cyclometalated gold(III) complexes with dithiocarbamate moiety
Summary
Platinum-based anticancer drugs have been developed during this time, and four platinum(II) drugs are approved for use in chemotherapy [4], cisplatin continues to be the most widely used together with the second-generation drug carboplatin [Pt(NH3 ) (CBDCA-O,O0 )]. Another important limitation of platinum drugs is the developing resistances shown by some kinds of tumors. The use of gold in medicine comes from its traditional use in medicine as antiarthritic agents such as gold(I) thiomalate (myocrisin), gold(I) thioglucose (solganol), and 2,3,4,6-tetra-o-acetyl-1-thio-b-D-glucopyranosato-(S)-triethylphosphine gold(I) (auranofin) (Figure 1) Some of these complexes, clinically established as antiarthritic gold(I)
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