Amino-substituted thalidomide analogs: Potent inhibitors of TNF-α production

Abstract Thalidomide, ( 1 ), is a known inhibitor of TNF-α release in LPS stimulated human PBMC. Herein we describe the TNF-α inhibitory activity of amino substituted analogs of thalidomide ( 1 ) and its isoindolin-1-one analog, EM-12 ( 2 ). The 4-amino substituted analogs were found to be potent inhibitors of TNF-α release in LPS stimulated human PBMC.