Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry

✍ Scribed by Michael A. Foley; Angela S. Hassman; David H. Drewry; David G. Greer; Craig D. Wagner; Paul L. Feldman; Judd Berman; D. Mark Bickett; Gerry M. McGeehan; Millard H. Lambert; Michael Green

• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 297 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(96)00333-2

✦ Synopsis

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.