Natural products and their synthetic derivatives have historically provided a rich source of pharmaceutical drug leads. Inspired by the application(s) of secondary metabolites in human disease, research in the Frederich laboratory focuses on developing new strategies and methods to prepare architecturally complex molecules that exhibit important biological activity in living systems. A critical aspect of this endeavor involves designing and understanding new reactions that build molecular complexity, thereby allowing us to approach challenging structures in a practical way. Access to targeted natural products and designed synthetic variants will open exciting avenues to explore their pharmacology. At this stage, exercises in molecular biology, biophysics and medicinal chemistry will become part of interdisciplinary research aimed at translating new discoveries in complex molecule synthesis to drug development.