Discovery Chemistry Congress Agenda

Registration

Bioorthogonal Palladium-Labile Prodrugs for Site-Specific Anticancer Therapy
Asier Unciti-Broceta, IGMM Academic Fellow, University of Edinburgh, United Kingdom

I will present the application of palladium-sensitive protecting groups as masking methods to eliminate the activity of chemotherapeutic drugs, while enabling the bioorthogonal rescue of the drugs’ pharmacological properties by heterogeneous palladium chemistry in cancer cell culture.

A Unified Approach to Lead-Oriented Synthesis
Richard Doveston, Researcher, Leeds University, United Kingdom

The concept of lead-oriented synthesis has recently captured the problems associated with sourcing large numbers of novel, diverse and lead-like small molecules for screening. Here we describe a unified approach that combines in silico library design and the development of synthetic methodologies to address this significant challenge.  

Coffee and Networking in Exhibition Hall

Exploring Protein-protein Interactions Using Scaffolded and Assembled Peptides as Synthetic Binding Site Mimics
Jutta Eichler, Professor, University of Erlangen-Nuremberg, Germany

Synthetic protein binding site mimics have proven excellent tools to explore protein-protein interactions. Such studies are aimed at providing insight into the structural and molecular details of these binding events, as well as to explore novel routes of therapeutic intervention.

A Structured Approach to Academic Drug Discovery
Simon Ward, Professor, University of Sussex, United Kingdom

Unmet medical need remains high but current big pharma business challenges are reducing research spend.  Our new model, staffed by former industry scientists, aims to address this gap in key therapeutic areas.

Lunch and Networking in Exhibition Hall

Poster Session

Exploring 3-D Pharmaceutical Space: Lead-oriented and Fragment-oriented Synthesis
Peter O'Brien, Professor, University of York, United Kingdom

This talk will cover two aspects: (i) the development of organolithium-mediated methodology for the synthesis of 3-D lead-like molecules; (ii) the development of an approach for the design and synthesis of 3-D fragment libraries.

Discovery of Potent and Selective Inhibitors of Monopolar Spindle 1 (MPS1) Kinase
Rob Montfort, Leader, The Institute of Cancer Research, United Kingdom

The talk focuses on the discovery of potent and selective MPS1 inhibitors, guided by structure-based design and cellular characterization of MPS1 inhibition, resulting in CCT251455, an attractive tool compound to further elucidate the therapeutic potential of MPS1 inhibition

Coffee and Networking in Exhibition Hall

Drug Discovery for Neglected Diseases
Ian Gilbert, Head of Chemistry, University of Dundee, United Kingdom

I will give a summary of the Drug Discovery Unit at the University of Dundee and outline some of the work that we have carried out on drug discovery for neglected tropical diseases.

Cancelled due to Travelling Problems
Wei Li, Associate Professor, Toho University, Japan

Natural products with great structural novelty and potent biological activity provide successful inspiration for new drug development. Herein, we present our new finding on natural compounds with unique chemical structure and potent bioactivity, indicating the potential for further drug development.

Drinks Reception

Choosing & Using Fragments in the Generation of Selective Kinase Inhibitors
Lee Walmsley, Senior Team Leader, Vernalis Ltd, United Kingdom

Choosing which fragments to progress into chemistry is a key determiner of success when generating quality leads. In this presentation I will present the approach taken by Vernalis in progressing fragment hits into series of efficient and selective kinase inhibitors.

Coffee and Networking in Exhibition Hall

Fragment-based Approach to Multi-target Compounds
Eugen Proschak, Professor, Goethe University, Germany

The rational development of multitarget drugs experiences an increased popularity since the past ten years. Application of fragment-based techniques to multitarget drug design might be the way to create interesting compounds with the desired polypharmacological profile.

Fragment-Based Drug Discovery Based on Diversity-Oriented Synthesis
Damian Young, Assistant Director, Center for Drug Discovery, Baylor College of Medicine, United States of America

The application of diversity-oriented synthesis(DOS) to fragment-based drug discovery (FBDD) provides enhanced opportunities for both the discovery of novel ligands to disease targets and their optimization to therapeutic leads.

Lunch and Networking in Exhibition Hall

Poster Session

The First Discovery of a Single Digit Nanomolar Small Molecule Blocker of a Protein-protein Interaction Target
Nils Hansen, Chief Executive Officer, Vipergen ApS, Denmark

Effective small molecule PPI blocker discovery using high fidelity DNA-encoded libraries and a low-noise homogeneous screening assay. The screen employs a unique principle of trapping small molecule binders together with the protein target in miniscule droplets.

Coffee and Networking in Exhibition Hall

Development of a Packed Bed Reactor for the Synthesis of Peptides and Foldamers: A Revolutionary Reduction of the Amino Acid Excess
Istvan Mandity, Head of Laboratory, University of Szeged, Hungary

A highly efficient continuous-flow technique for the synthesis of peptides was developed which allows the application of only 1.5 equivalents of amino acids during coupling, while yielding virtually quantitative conversions. Difficult sequences and ß-peptide foldamers with alicyclic side-chains were synthesized in excellent yields.

Close of Conference