Small-molecule drugs, including natural products, have been the cornerstone of medicine and have had a significant impact on shaping our world. Expanding the structural complexity and improving therapeutic efficacy presents a set of unique synthetic chemistry challenges. Working with partners at TMC, organic and synthetic chemists at Rice will collaborate to create new synthetic and naturally derived drugs using cutting-edge synthetic and mechanistic methods (e.g. enzymatic solutions for complex organic reactions) and to integrate small-molecular concepts into larger-scale drug conjugates (e.g. creating precise antibody drug conjugates) that can be readily tested in clinical settings.