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Details of Grant 

EPSRC Reference: GR/S06431/01
Title: Completion of our Convergent Approach to Eleutherobin-A Marine Natural Product with Taxol-Like Activity
Principal Investigator: Mann, Professor J
Other Investigators:
Researcher Co-Investigators:
Project Partners:
Department: Sch of Chemistry and Chemical Eng
Organisation: Queen's University of Belfast
Scheme: Standard Research (Pre-FEC)
Starts: 01 July 2003 Ends: 31 December 2004 Value (£): 85,472
EPSRC Research Topic Classifications:
Biological & Medicinal Chem. Chemical Synthetic Methodology
EPSRC Industrial Sector Classifications:
Healthcare Pharmaceuticals and Biotechnology
No relevance to Underpinning Sectors
Related Grants:
Panel History:  
Summary on Grant Application Form
The marine natural product eleutherobin stabilises microtubules against depolymerisation and thus inhibits mitosis. It shares this mode of action with taxol, the epothilones, and other natural products, but appears to be more potent. It has been the subject of two linear total syntheses, but has never been prepared by an economically viable convergent route. The aim of the project is to achieve this goal with a synthetic route that is flexible enough to provide ready access to a wide range of novel structures.The route proceeds via two key intermediates which can be produced in six linear steps, and we propose to investigate a variety of strategies for joining these subunits to produce the basic skeleton of eleutherobin in no more than six further steps.We then aim to complete the synthesis of both the natural product and structural analogues for biological evaluation. Our close collaboration with the Department of Oncology will ensure that lead compounds are identified and can then be taken on for pre-clinical evaluation.
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Organisation Website: http://www.qub.ac.uk