Author/Authors :
Michael A. Foley، نويسنده , , Angela S. Hassman، نويسنده , , David H. Drewry، نويسنده , , David G. Greer، نويسنده , , Craig D. Wagner، نويسنده , , Paul L. Feldman، نويسنده , , Judd Berman، نويسنده , , D. Mark Bickett، نويسنده , , Gerry M. McGeehan، نويسنده , , Millard H. Lambert and H. Eric Xu، نويسنده , , Michael Green، نويسنده ,
Abstract :
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.