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

…, RT Patterson, Y Chen, G Kaplan, DI Stirling

Index: Muller, George W.; Chen, Roger; Huang, Shaei-Yun; Corral, Laura G.; Wong, Lu Min; Patterson, Rebecca T.; Chen, Yuxi; Kaplan, Gilla; Stirling, David I. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 11 p. 1625 - 1630

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Citation Number: 313

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.