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

  • Bioorg Med Chem Lett. 1999 Jun 7;9(11):1625-30. doi: 10.1016/s0960-894x(99)00250-4.
G W Muller  1 ,  R Chen ,  S Y Huang ,  L G Corral ,  L M Wong ,  R T Patterson ,  Y Chen ,  G Kaplan ,  D I Stirling
Affiliations
  • 1. Celgene Corporation, Warren, NJ 07059, USA.
PMID: 10386948 DOI: 10.1016/s0960-894x(99)00250-4
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.

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