Mj. Stocks et al., THE CONTRIBUTION TO BINDING OF THE PYRANOSIDE SUBSTITUENTS IN THE EXCISED BINDING DOMAIN OF FK-506, Bioorganic & medicinal chemistry letters, 4(12), 1994, pp. 1457-1460
The contributions of the C-ll methyl and C-13 / C-15 methoxy substitue
nts to the affinity of FK-506 for the immunophilin FKBP-12 were invest
igated. Subtraction of the C-11 methyl group led to a 400-fold drop in
affinity. Removal of the C-13 and C-15 methoxy substituents led to a
much smaller drop in affinity.