The revolution in biology over the past two decades has resulted in radical new opportunities for discovery of new drugs. Most importantly, it has defined major drug targets in the form of molecular components of disease processes. In recent years, there is a growing pressure on the pharmaceutical industries to increase the efficiency with which novel leads are generated and screened for biological activity. Natural products have served as a major source of drugs for centuries, and about half of the pharmaceuticals in use today are derived from natural products. Nature is unrivalled in its ability to produce organic molecules with structural complexity and biological potency; thus nature has been performing combinatorial chemistry for thousands of years. Interest in natural products research within the new era of drug research is strong and can be attributed to several factors. These include issues like unmet medical needs, diversity of both chemical structures and biological activities, the utility of bioactive natural products as biochemical and molecular probes, the development of novel and sensitive techniques to detect biologically active natural products, improved techniques to isolate, purify, and structurally characterise the active constituents. The opportunities within the new era of drug discovery and development, for multidisciplinary research that joins the forces of natural product chemistry, molecular and cellular biology, synthetic and analytical chemistry, biochemistry, and pharmacology to exploit the diversity of chemical structures and biological of natural products, are immense.