Natural products (secondary metabolites; naturally occurring small organic molecules) continue to play a pivotal role in modern drug discovery since they are superior new drug leads compared with purely synthetic compounds (hit rates of ~0.3% vs. <0.001%, respectively). Interestingly however, in most cases the active ingredient of the end-product (drug) is not a natural product but rather a semisynthetic modification or a totally synthetic compound with a natural product-inspired pharmacophore.¹ This highlights the importance of modern synthetic organic chemistry in the exploitation of natural products. On the other hand, natural products, with their diverse and often complex structures and important biological activity, historically define the state of the art of organic chemistry. Today, they continue to drive basic research in synthetic organic chemistry (for the discovery and validation of new methods and strategies)² and are valuable tools for Chemical Biology (i.e., the exploration of biological systems using chemistry techniques).³

In this context and aiming to facilitate further exploitation of bioactive natural products, objectives of this group are:

• The total synthesis of natural products with important biological activities.
• The design, synthesis and study of designed analogues thereof.
• The training of young researchers in the “Art and Science” of Natural Products Synthesis.

In parallel, the expertise of the team in the design and synthesis of complex organic molecules is exploited for:

• The preparation of organic molecules with possible technological applications (e.g., photoresist etch enhancement additives, linkers for the preparation of polymers).

References

1. J.W.H. Li, J.C. Vederas, Science 2009, 325, 161; G.M. Cragg, et al., Chem. Rev. 2009, 109, 3012; D.J. Newman, G.M. Cragg, J. Nat. Prod. 2007, 70, 461.
2. K.C. Nicolaou, S.A. Snyder, Classics in total synthesis II, WILEY-VCH Verlag GmbH & Co., Weinheim, Germany, 2003; K.C. Nicolaou, E.J. Sorensen, Classics in total synthesis, VCH Publishers, Inc., New York (USA), 1996.
3. Editorial, “The state of the art of chemical biology”, ChemBioChem 2009, 10, 16.