Author/Authors :
John C. McKew، نويسنده , , Frank Lovering، نويسنده , , James D. Clark، نويسنده , , Jean Bemis، نويسنده , , YiBin Xiang، نويسنده , , Marina Shen، نويسنده , , Wen Zhang، نويسنده , , Juan C. Alvarez، نويسنده , , Diane Joseph-McCarthy، نويسنده ,
Abstract :
An SAR effort focused on generating cPLA2α inhibitors using a substrate mimetic approach is reported. Indole inhibitors of cPLA2α with promising pharmacokinetic parameters that were active in both an isolated enzyme assay and in cell-based assays were discovered. Modeling these compounds into the cPLA2α structure validated the assumptions made at the start of the SAR effort
