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Abstract
Novel enediyne-amino acid conjugates 1-4 have been synthesized. All of these effectively
target the enzyme chymotrypsin inhibiting its proteolytic activity. The conjugate
with a directly linked phenyl alanine is the most effective inhibitor with a K(i)
of 3 microM. The mode of inhibition is mostly competitive or of a mixed type depending
on the nature of the inhibitor.