Friday 25 September
The ready availability of structurally novel lead molecules with appropriately controlled molecular properties (e.g. logP, molecular weight and fraction of sp3 atoms) is crucial to the ability of the pharmaceutical industry to bring new small molecule drugs to market. However, it is now recognised that access to such lead molecules is poorly served not only by many current commercial libraries but also by the synthetic methods widely adopted within industry and many of those developed in academic laboratories. In this meeting, approaches to rectifying this issue will be presented both from academia and industry, with the hope of stimulating a broader recognition of, and solutions to, the challenges of lead-oriented synthesis.
Meeting report: open in a new window
Program:
| 09:45 | Registration and coffee |
| 10:30 | Welcome and housekeeping |
| Prof. Adam Nelson (University of Leeds) | |
| 10:40 | How synthetic chemistry can drive the discovery of drugs of the future |
| Dr Ian Churcher (GSK) | |
| 11:00 | Exploring 3D pharmaceutical space: lead-oriented and fragment-oriented synthesis |
| Prof. Peter O’Brien (University of York) | |
| 11:40 | LLAMA: An open-access tool to guide lead-oriented synthesis |
| Prof. Adam Nelson (University of Leeds) & Dr Richard Doveston (TU Eindhoven) | |
| 12:00 | Lunch and freeware demonstration |
| 13:15 | Synthetic strategies for the efficient exploration of lead-like space |
| Prof. Steve Marsden (University of Leeds) | |
| 13:55 | Design and exploitation of novel medicinal chemistry reagent sets |
| Dr Jason Kettle (AstraZeneca) | |
| 14:35 | Enriching chemical space to drug undruggable targets |
| Prof. David Spring (University of Cambridge) | |
| 15:15 | Afternoon refreshments |
| 15:45 | Cross coupling 2.0 |
| Prof Jeffrey Bode (ETH Zurich) | |
| 16:45 | Concluding remarks and close of meeting |
Organising Committee: Prof Steve Marsden & Prof Adam Nelson
