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

1999; Elsevier BV; Volume: 9; Issue: 11 Linguagem: Inglês

10.1016/s0960-894x(99)00250-4

1464-3405

George W. Muller, Roger Chen, Shaei‐Yun Huang, Laura G. Corral, Lu Min Wong, Rebecca T. Patterson, Yuxi Chen, Gilla Kaplan, David Stirling,

Protein Kinase Regulation and GTPase Signaling

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.