Potent small molecule inhibitors of spleen tyrosine kinase (Syk).

  title={Potent small molecule inhibitors of spleen tyrosine kinase (Syk).},
  author={Justine Y Q Lai and Paul J Cox and Rajesh I. Patel and Shazia Sadiq and David J Aldous and Sukanthini Thurairatnam and Keith C. Smith and Darren Wheeler and Savita Jagpal and Sofia Parveen and Gary Fenton and Trevor K P Harrison and Clive McCarthy and Paul Bamborough},
  journal={Bioorganic & medicinal chemistry letters},
  volume={13 18},
A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/Fc epsilon RI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC(50)=5 nM, EC(50)=1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar Surface Area was lowered to <110 A(2), leading to the identification of amide 32 (IC(50)=145 nM, EC(50)=100 nM). 

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