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Synthesis and bio-assay of RCM-derived Bowman–Birk inhibitor analogues

Org. Biomol. Chem., 2004,2, 281-283  2012/6/20 1:55:59

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 Ki 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.



 

 Graphical abstract: Synthesis and bio-assay of RCM-derived Bowman–Birk inhibitor analogues
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