The importance of drug discovery and development to better the quality of life for mankind has been realized for decades. Natural products, regardless of their origin, are an important source of chemically and therapeutically useful scaffolds for drug discovery. However, establishing such a sustainable program in Thailand has presented itself as a true challenge and a frontier to push forward. Medicinal chemistry research in our laboratory encompasses several different classes of biologically active frameworks. Development of novel synthetic methodologies, which are short, simple, high-yielding, economical, and environmentally friendly, represents not only an academic but also a practical challenge.