Dr. Andrea TrabocchiAssociate Professor of Organic Chemistry
Department of Chemistry “Ugo Schiff”, University of Florence, Italy
Speech Title: Diversity-Oriented Synthesis of sp3-rich molecular scaffolds as a tool for chemical genetics
Abstract: Chemical genetics is a powerful approach in early drug discovery for identifying small molecules with the ability to induce a biological phenotype or to interact with a particular gene product. Hence, efficient and versatile synthetic processes capable of generating complex and diverse molecular libraries are in demand, and Diversity-Oriented Synthesis (DOS) of small molecules is the concept of choice to give access to new chemotypes with high chemical diversity and complexity. The implementation of this technology starting from carbohydrates and amino acids is poorly investigated, and in this view we explore suitable chemistry from such natural product precursors to obtain novel heterocyclic sp3-rich molecular structures without the need of transitional protection/deprotection stages. Chemoinformatics characterization of new molecules in the context of chemical space and application in cell-based phenotypic assays are provided to select valuable candidates for subsequent medicinal chemistry follow-up and mechanistic elucidation.
Biography: Andrea Trabocchi is Associate Professor of Organic Chemistry at the University of Florence, Italy, where his research is focused in the area of diversity-oriented synthesis and peptidomimetic chemistry with applications in the discovery of therapeutics for Alzheimer’s disease, cancer and infectious diseases. He is also involved in molecular imaging as deputy director of a preclinical imaging center at University of Florence. He obtained a PhD in Chemical Sciences from the University of Florence, and received training on peptide chemistry at the Imperial College, UK. He authored about 90 papers and filed 4 patents on small molecule synthesis and biomedical applications. Editorial appointments include three books on Diversity-Oriented Synthesis, Peptidomimetics, and Small Molecule Drug Discovery.