title: Amino-substituted thalidomide analogs: potent inhibitors of TNF-alpha production.
abstract: 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.
authors.affiliation: Celgene Corporation, Warren, NJ 07059, USA.
authors.forename: G W
authors.initials: GW
authors.lastname: Muller
authors.forename: R
authors.initials: R
authors.lastname: Chen
authors.forename: S Y
authors.initials: SY
authors.lastname: Huang
authors.forename: L G
authors.initials: LG
authors.lastname: Corral
authors.forename: L M
authors.initials: LM
authors.lastname: Wong
authors.forename: R T
authors.initials: RT
authors.lastname: Patterson
authors.forename: Y
authors.initials: Y
authors.lastname: Chen
authors.forename: G
authors.initials: G
authors.lastname: Kaplan
authors.forename: D I
authors.initials: DI
authors.lastname: Stirling
mesh_terms: 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
chemical_list: D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide