Amino-substituted thalidomide analogs: potent inhibitors of TNF-alpha production.
Thalidomide, (1), is a known inhibitor of TNF-alpha release in LPS stimulated human PBMC. Herein we describe the TNF-alpha 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-alpha release in LPS stimulated human PBMC.
Muller
G W
GW
Celgene Corporation, Warren, NJ 07059, USA.
Chen
R
R
Huang
S Y
SY
Corral
L G
LG
Wong
L M
LM
Patterson
R T
RT
Chen
Y
Y
Kaplan
G
G
Stirling
D I
DI
D001769:Blood / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D013329:Structure-Activity Relationship; D013792:Thalidomide / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*; D020298:U937 Cells
D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide