Although combinatorial chemistry technology has enabled large libraries of compounds to be screened for biological activity and synthetic modifications to be effected rapidly, the reality is that quality leads and development candidates for many drug targets still prove difficult to find. This is particularly relevant to antiinfective, oncology, and immunomodulation targets and also those involving protein–protein interactions. In the past, natural products have led to excellent drugs for precisely these therapeutic areas, but the difficulties of identifying and utilising such compounds compared to less complex molecules synthesised using combinatorial chemistry techniques then led many to question their value in modern-day drug discovery. In fact, in the early 1990s, a significant number of pharmaceutical companies reduced or even terminated the natural product-based drug discovery activities that had served them so well in the past. Nevertheless a renaissance appears to be at hand. The pressing need to fill drug development pipelines, combined with attractive outsourcing opportunities, have prompted many of the very same companies to reevaluate the utility of natural products as sources of novel drug leads. Through a judicious combination of new technologies and compelling business model, at least one Singapore-based company is offering cost-effective solutions for accessing the unique chemical diversity found in Nature. Drug Dev. Res. 62:362–370, 2004. © 2004 Wiley-Liss, Inc.