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 μM. The mode of inhibition is mostly competitive or of a mixed type depending on the nature of the inhibitor.