Author/Authors :
John L. Gilmore، نويسنده , , Bryan W. King، نويسنده , , Naoyuki Asakawa، نويسنده , , Kimberly Harrison، نويسنده , , Andrew Tebben، نويسنده , , James E. Sheppeck II، نويسنده , , Ruiqin Liu، نويسنده , , Maryanne Covington، نويسنده , , James J. -W. Duan، نويسنده ,
Abstract :
A novel series of TNF-α converting enzyme (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds use a triazolethione moiety as the zinc binding ligand and exhibit IC50 values from 1.5 to 100 nM in a porcine TACE assay. They also have excellent selectivities over other MMPs.