Metal complexes of saccharin and thiosaccharin as potential anticancer and antimicrobial agents

Based on the chemotherapeutic success of cisplatin, carboplatin and oxaliplatin as anticancer drugs, and silver sulfadiazine (AgSDZ) as an antibacterial drug, exploration of the anticancer and antibacterial potential of new metal complexes has received increasing attention during the last three decades. Saccharin (sacH) is a well-known worldwide artificial sweetener. Its deprotonated form (sac) is a polyfunctional ligand, coordinating to different metals due to the presence of hard and soft donor sites (see comment below). In the last two decades, a large number of mixed-ligand metal complexes containing sac and tsac ligands have been synthesized and in some cases, they have demonstrated better in vitro and in vivo biological activities than approved standard drugs. This review describes the design, anticancer and antimicrobial activity screening of metal complexes of sac and its thio derivative (tsac) as prospective drug candidates. The metal sac complexes herein are categorized according to the ancillary ligands present in the complexes, and their anticancer and antimicrobial activities are discussed in detail. The main molecular targets and cellular pathways involved in the mechanism of action of the metal complexes were also explored. The growing field demonstrates promising in vitro and in vivo results with a significant interest for future research in medicinal inorganic chemistry. • Anticancer activity of metal complexes of saccharin and thiosaccharin are highlighted. • Metal complexes of saccharin demonstrate potent in vitro and in vivo activity. • Antimicrobial activity of metal complexes of saccharin and thiosaccharin are introduced. • Metal complexes of saccharin exhibit antibacterial, antifungal and antiviral activity.