New thalidomide analogues derived through Sonogashira or Suzuki reactions and their TNF expression inhibition profiles

…, SL Ng, ME Polomska, M Karimi, LJ Abraham

Index: Stewart, Scott G.; Braun, Carlos J.; Ng, Sze-Ling; Polomska, Marta E.; Karimi, Mahdad; Abraham, Lawrence J. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 2 p. 650 - 662

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Citation Number: 19

Abstract

A library of new thalidomide C4/5 analogues containing either a phenyl or alkyne tether were synthesized using Sonogashira or Suzuki cross coupling reactions from their aryl halogenated precursors. All thalidomide analogues were tested for their ability to inhibit the expression of the proinflammatory cytokine Tumor Necrosis Factor (TNF). More explicitly the use of a novel reporter system utilizing the promoter region of the TNF gene in a human T- ...