Coordination compounds offer a flexible framework for the thoughtful design of novel therapeutic-metallodrugs because of the unique properties of metal ions, such as their ability to coordinate with a wide range of organic ligands, variable oxidation states, a wide range of geometries, and coordination numbers. The pharmaceutical potential of a metal ion and associated substances is validated by the prevalence of various disease states linked to a metal ion's excess or deficiency within the biological system. Researchers have sought more selective, efficacious metallodrugs that cause fewer adverse effects. Attempts have resulted in considering a large range of organic ligands, preferably polydentate ligands with demonstrated biological activity, and a large range of metals from the periodic table, primarily from the d-block. In this review, we have outlined the key coordination complexes comprising N-, O-, and S-donor ligands reported in the last six years to demonstrate the potential applications of these metallo-organic complexes. The synthetic pathways of ligands, their complexes, and their potential for therapeutic applications are highlighted.