Australia is rich in plant, animal and microbial biodiversity, inhabiting geographically diverse ecosystems from the northern tropics to southern temperate zones, and as far south as Antarctica. Our research aims to explore this remarkable living resource, to discover new molecules and knowledge that inform and inspire the development of new and improved pharmaceuticals, as well as chemicals for use in agriculture and research. Some therapeutic targets include neurodegenerative (i.e. Alzheimer’s, Parkinson’s) and infectious diseases, as well as cancer, diabetes and pain. We also target new chemicals to treat highly drug-resistant parasites in livestock, and explore chemical ecology as a means to develop natural solutions to control the impact of invasive pests (i.e. cane toads) on Australian ecosystems. To achieve these goals we have assembled core expertise and infrastructure in organic, analytical, chromatographic, spectroscopic and synthetic chemistry, allowing us to discover a wide diversity of molecules, rich in unusual carbon skeletons, heterocycles and functionality, derived from the full array of known and new biosynthetic pathways. Strategic alliances further extend our capability into the disciplines of zoology, ecology and microbiology, as well as cell and molecular biology, pharmacology and biochemistry.