Thalidomide, (1), is a known inhibitor of TNF-alpha release in LPS stimulat
ed human PBMC. Herein we describe the TNF-alpha inhibitory activity of amin
o substituted analogs of thalidomide (1) and its isoindolin-1-one analog, E
M-12 (2). The 4-amino substituted analogs were found to be potent inhibitor
s of TNF-alpha release in LPS stimulated human PBMC. (C) 1999 Elsevier Scie
nce Ltd. All rights reserved.