Activity-directed synthesis toolkit

Lead Research Organisation: University of Leeds
Department Name: Sch of Chemistry

Abstract

Activity-directed synthesis (ADS) is a novel discovery approach in which bioactive small molecules emerge in parallel with an associated synthetic route. The approach deliberately exploits reactions with many possible outcomes. Reaction arrays are performed in plate-based format, and the crude product mixtures are assayed for biological activity. Promising reactions then inform the design of reaction arrays in subsequent rounds. Finally, optimised reactions are scaled up, and the bioactive products are purified, structurally elucidated and functionally characterised. This iCASE project (in collaboration with GSK) will focus on expansion of the reaction toolkit for ADS to enable scaffold hopping. The new chemical tools will be exploited in the ADS of small molecule modulators of exemplar protein targets. The project focuses on the development of a new chemical approach to drive ligand discovery, and aligns with the EPSRC's chemical biology research area.

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/N509243/1 30/09/2015 31/12/2021
1799580 Studentship EP/N509243/1 30/09/2016 29/09/2020 Adam Ieuan Green
EP/P510555/1 30/09/2016 29/09/2021
1799580 Studentship EP/P510555/1 30/09/2016 29/09/2020 Adam Ieuan Green
 
Description Activity-directed synthesis toolkit
Amount £90,584 (GBP)
Funding ID 1799580 
Organisation Engineering and Physical Sciences Research Council (EPSRC) 
Sector Public
Country United Kingdom
Start 09/2016 
End 09/2020