| EPSRC Reference: |
GR/M59488/01 |
| Title: |
SOLID PHASE SYNTHESIS OF CARBOHYDRATE-MODIFIED HETEROCYCLIC LIBRARIES |
| Principal Investigator: |
Kellam, Professor B |
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| Department: |
Sch of Pharmaceutical Sciences |
| Organisation: |
University of Nottingham |
| Scheme: |
Standard Research (Pre-FEC) |
| Starts: |
20 September 1999 |
Ends: |
19 September 2000 |
Value (£): |
51,874
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| EPSRC Research Topic Classifications: |
| Biological & Medicinal Chem. |
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| EPSRC Industrial Sector Classifications: |
| No relevance to Underpinning Sectors |
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Summary on Grant Application Form |
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This project will develop a novel solid-phase synthetic strategy for the construction of a peptoid and carbohydrate functionalised tetrahydroisoquinoline library. Using appropriate biological assays, the library will be employed to identify the most potent angiogenesis inhibitors from the original members. Proliferation of solid tumours and metastases is dependent tetrasaccharide region of new blood vessels; termed angiogenesis. Mimetics of a common terminal tetrasaccharide region of many cellular glycoproteins and glycolipids (sialyl Lewis X), have been demonstrated to inhibit angiogenesis both in vitro and in vivo, and this may herald new drug entities for the treatment of cancer.Molecular modelling studies within our laboratories have identifies for the tetrahydroisoquinoline structure as an excellent template on which to explore new sialyl Lewis X mimetics using a cominatorial approach. Therefore, a 600-member library will be constructed around the aforementioned heterocyclic template, using novel synthetic building blocks and commercially available compounds.The most active members of the library will be identified using the chick chorioallantoic membrane biological assay. This collaborative arm of the project work will be undertaken at the Institute of Cancer Research, London under the guidance of Dr Chris Boshoff.
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Key Findings |
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This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
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Potential use in non-academic contexts |
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This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
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Impacts |
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| Description |
This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk |
| Summary |
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| Date Materialised |
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Sectors submitted by the Researcher |
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This information can now be found on Gateway to Research (GtR) http://gtr.rcuk.ac.uk
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| Project URL: |
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| Further Information: |
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| Organisation Website: |
http://www.nottingham.ac.uk |