bacteria to established drugs is a major health concern. Antibiotics can interact with a variety of biomolecules, which may result in inhibition of the biochemical or biophysical processes associated with the biomolecules. Metal complexes of antibiotics in particular offer great promise for such novel activity. Metalloantibiotics is a broad logical term, many metalloantibiotics derivatives and metal complexes of synthetic ligands and donors demonstrating antibacterial, antiviral, and antineoplastic activities were included. In this review, we focus on few synthetic metalloantibiotics to provide a view of the term ‘‘metalloantibiotics.’’ Metal ions play a key role in the actions of synthetic and natural metalloantibiotics, and are involved in specific interactions of these antibiotics with proteins, membranes, nucleic acids, and other biomolecules including DNA, RNA, proteins, receptors, and lipids.