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Synthesis and bio-assay of RCM-derived Bowman-Birk inhibitor analogues
Steven M Miles1, Robin J Leatherbarrow, Stephen P Marsden
1Department of Chemistry, Imperial College London, South Kensington Campus, London, UKSW7 2AZ.
Abstract:
Bowman-Birk inhibitor analogues containing 2, 3 and 4-carbon analogues of the natural disulfide were synthesised via solid phase microwave-assisted RCM and found to have K(i) values against chymotrypsin in the low to sub-micromolar range, the best replacement for the disulfide arising from the linkage by RCM of two l-homoallylglycine residues.
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