This review article summarizes recent applications of electrochemical techniques to redox-active drug development and mechanistic studies. It includes a general introduction to the use of electrochemistry in biology, with a focus on how electrochemistry can uniquely provide both kinetic and thermodynamic information. A number of studies are reported from the literature and the authors' laboratories, including the investigation of reactive oxygen species, biooxidative/bioreductive activation of pro-drugs, and DNA alkylation, with a particular emphasis on quinones and related compounds. Data from techniques ranging from traditional cyclic voltammetry to sophisticated single cell studies are presented. The examples herein presented illustrate how electrochemical, biochemical and medical knowledge can be integrated to develop strategies for the design and development of redox-selective therapeutics.