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Bioorg Med Chem Lett. 2003 Sep 15;13(18):3111-4.

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

Author information

1
Aventis Pharmaceuticals, Route 202/206, Brigdewater, NJ 08807, USA.

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).

PMID:
12941345
DOI:
10.1016/s0960-894x(03)00658-9
[Indexed for MEDLINE]

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