Potent small molecule inhibitors of spleen tyrosine kinase (Syk)

Autor: Darren Wheeler, Gary Fenton, Bamborough Paul Lindsay, Paul Joseph Cox, Sukanthini Thurairatnam, David J. Aldous, Rajesh Patel, Lai Justine Yeun Quai, Sofia Parveen, Trevor K.P. Harrison, Keith Smith, Clive Mccarthy, Shazia Sadiq, Savita Jagpal
Rok vydání: 2003
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 13:3111-3114
ISSN: 0960-894X
Popis: A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/FceRI 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 2 , leading to the identification of amide 32 (IC 50 =145 nM, EC 50 =100 nM).
Databáze: OpenAIRE