Stereoselective Synthesis of Bioactive Compounds (Track)

EXPLORING NOVEL CHEMICAL SCAFFOLDS WITH THE EUROPEAN LEAD FACTORY

Andrew Nortcliffe

School of Chemistry, University of Nottingham, UK

Abstract

The European Lead Factory is a €200M pan-European platform for drug discovery supported by the Innovative Medicines Initiative (IMI). The aim of the project, to prepare a novel library of 500,000 'drug-like' compounds to be screened for the development of potential new medicines and openly available for the public sector. The project is a joint venture between major pharmaceutical companies, drug discovery SME's and academic research groups across Europe.

At the University of Nottingham a team of 12 postdocs are involved in the design and validation of novel chemical scaffolds to be used in library production. The aim of the work is to provide chemically diverse, sp³ rich scaffolds that can be prepared rapidly and on scale. Many of the prepared scaffolds utilise chemistry that is widely overlooked in the mainstream of drug synthesis including diazocarbonyl chemistry, Diels-Alder reactions, nitrone-alkene cycloadditions and tandem condensation/cycloadditions.

Presented here today are some of the success stories from our work from the past two years.

Keywords: European Lead Factory, sp³ scaffolds, high-throughput screening.