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.

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.

MeSH terms

  • Blood / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • Structure-Activity Relationship
  • Thalidomide / analogs & derivatives*
  • Thalidomide / chemical synthesis*
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*
  • U937 Cells

Substances

  • Tumor Necrosis Factor-alpha
  • Thalidomide