Reactive oxygen species (ROS) (H2O2, OCl−, ĽOH, O2−) are a family of reactive molecules that are generated intracellularly and are engaged in many biological processes. In physiological concentrations, ROS act as signaling molecules to a number of metabolic pathways; however, in excess they can be harmful to living organisms. Overproduction of ROS has been related to many pathophysiological conditions and a number of studies have been reported in elucidating their mechanism in these conditions. With the aim of harnessing this role, a number of imaging tools and therapeutic compounds have been developed. Here these imaging and therapeutic tools are reviewed and particularly those structures with ROS-sensitivity based on their biomedical applications and their functional groups. There is also a brief discussion about the method of preparation as well as the mechanism of action.