| Literature DB >> 12941345 |
Justine Y Q Lai1, Paul J Cox, Rajesh Patel, Shazia Sadiq, David J Aldous, Sukanthini Thurairatnam, Keith Smith, Darren Wheeler, Savita Jagpal, Sofia Parveen, Gary Fenton, Trevor K P Harrison, Clive McCarthy, Paul Bamborough.
Abstract
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).Entities:
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Year: 2003 PMID： 12941345 DOI： 10.1016/s0960-894x(03)00658-9
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823