Novel Polyfunctional 3D Scaffolds for Drug Discovery

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

Abstract

The pharmaceutical industry relies upon the commercial availability of small polyfunctional building blocks from which to generate high quality screening libraries. The vast majority of those currently available are two-dimensional in nature, despite strong evidence that three-dimensionality is highly advantageous in drug candidates.
In this project, the chemoinformatic tool LLAMA (developed at Leeds) will be used to prioritise the synthesis of a number of novel, small, polyfunctional and highly 3D scaffolds. These compounds will then be decorated to provide small libraries of high quality fragments and screening compounds. The candidate compounds will be exposed to a range of screens to demonstrate biological relevance. Process optimisation of key compounds will be performed and, where appropriate, will be investigated for tech transfer towards commercialisation.

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/N509681/1 01/10/2016 30/09/2021
1939686 Studentship EP/N509681/1 01/10/2017 31/03/2021 Scott Rice