Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3, 4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents

…, I Sienaert, J Herman, G Clydesdale, H Sefrioui…

Index: De Jonghe, Steven; Marchand, Arnaud; Gao, Ling-Jie; Calleja, Agnes; Cuveliers, Eva; Sienaert, Ilse; Herman, Jean; Clydesdale, Gavin; Sefrioui, Hassane; Lin, Yuan; Pfleiderer, Wolfgang; Waer, Mark; Herdewijn, Piet Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 145 - 149

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Citation Number: 11

Abstract

Screening of a pteridine-based compound library led to the identification of compounds exhibiting immunosuppressive as well as anti-inflammatory activity. Optimization afforded a series of 2-amino-4-N-piperazinyl-6-(3, 4-dimethoxyphenyl) pteridine analogues. The most potent congeners in this series displayed low nM IC50 values in the Mixed Lymphocyte Reaction (MLR) assay. In addition, these compounds also have potent anti-inflammatory ...