How Best Can Synthesis Support Bioactive Molecule Discovery? Seminar

The discovery of bioactive small molecules is an enduring theme in medicinal chemistry and chemical biology. In this talk, three distinct approaches to the exploration of chemical space will be presented. First, an approach to the synthesis of natural product-like molecules with unprecedented scaffold diversity will be outlined. Second, an approach to the synthesis of lead-like molecular scaffolds will be described. Finally, a novel approach - which we have termed activity-directed synthesis - will be described in which the emergence of the synthetic route is guided solely by the bioactivity of the resulting products.