Synthetic FKBP12 ligands. Design and synthesis of pyranose replacements

A number of FKBP12 ligands were designed and synthesised and their affinity for FKBP12 assessed. In these ligands the pyranose ring of FK506 was replaced by other more synthetically accessible groups. The preparation of suitable intermediates for the synthesis of “dual domain” inhibitors (compounds...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1994-11, Vol.4 (21), p.2501-2506
Main Authors: Birkenshaw, Timothy N., Caffrey, Moya V., Cladingboel, David E., Cooper, Martin E., Donald, David K., Furber, Mark, Hardern, David N., Harrison, Richard P., Marriott, David P., Perry, Matthew W.D., Stocks, Michael J., Teague, Simon J., Withnall, W.John
Format: Article
Language:English
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Summary:A number of FKBP12 ligands were designed and synthesised and their affinity for FKBP12 assessed. In these ligands the pyranose ring of FK506 was replaced by other more synthetically accessible groups. The preparation of suitable intermediates for the synthesis of “dual domain” inhibitors (compounds 6a–c, 15 and 22) is also described. A number of FKBP12 ligands were synthesised and their affinity for FKBP12 assessed. The preparation of suitable intermediates for the synthesis of ‘dual domain’ inhibitors is also described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80272-9