The use of Australian-sourced biota for natural products drug discovery and chemical biology research has a strategic advantage, since this unique resource has only been superficially explored for new pharmaceutical agents and chemical probes. This presentation will: (i) give a brief overview of NatureBank - a unique biodiscovery platform based on natural product extracts and fractions derived from Australian plants, fungi and marine invertebrates; (ii) describe the identification and biology associated with several new natural products that have recently been discovered by the Davis group and their potential impact to the field of biodiscovery; and (iii) detail the design and synthesis of several novel libraries that were created using isolated natural product scaffolds and semisynthetic methodology.