Due to their diverse pharmacological properties, triazoles are important tools in medicinal chemistry and may be involved in many cancer-related pathways. Structural modifications of this molecule can be useful in drug development. Although research efforts are directed toward the development of synthetic triazole analogs, much work needs to be done in this area of drug discovery. Medicinal chemists are interested in generating new triazole derivatives because of the potential therapeutic uses of these compounds. This chapter covers the general chemistry, methods of synthesis, and specific pharmacological actions of the triazole core. Data on commercially available clinical and investigational triazole compounds are also included. The purpose of this chapter is to increase recognition of the importance of these heterocycles through the design and synthesis of new triazole derivatives with advanced and unexplored pharmacological implications.