Rapid Synthesis Of Novel Dipeptide Inhibitors Of Human Collagenase And Gelatinase Using Solid Phase Chemistry

Solid phase chemistry expedited the systematic modification of the C and N-terminal groups of cysteine derived lead compound 1 (collagenase IC50 63nM), providing a series of matrix metalloproteinase inhibitors. Potent inhibitors of collagenase (1-2, 4-6, and 10-13) and gelatinase (4-8) were identified. Insights into the binding mode of selective inhibitors will be discussed. Copyright (C) 1996 Elsevier Science Ltd