Design and synthesis of enediyne-peptide conjugates and their inhibiting activity against chymotrypsin.

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.