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

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

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JONGHE, Steven De, Arnaud MARCHAND, Ling-Jie GAO, Agnes CALLEJA, Eva CUVELIERS, Ilse SIENAERT, Jean HERMAN, Gavin CLYDESDALE, Hassane SEFRIOUI, Yuan LIN, Wolfgang PFLEIDERER, Mark WAER, Piet HERDEWIJN, 2011. Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents. In: Bioorganic & Medicinal Chemistry Letters. 21(1), pp. 145-149. ISSN 0960-894X. eISSN 1464-3405. Available under: doi: 10.1016/j.bmcl.2010.11.053

@article{Jonghe2011-01-01Synth-19906, title={Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents}, year={2011}, doi={10.1016/j.bmcl.2010.11.053}, number={1}, volume={21}, issn={0960-894X}, journal={Bioorganic & Medicinal Chemistry Letters}, pages={145--149}, author={Jonghe, Steven De and Marchand, Arnaud and Gao, Ling-Jie and Calleja, Agnes and Cuveliers, Eva and Sienaert, Ilse and Herman, Jean and Clydesdale, Gavin and Sefrioui, Hassane and Lin, Yuan and Pfleiderer, Wolfgang and Waer, Mark and Herdewijn, Piet} }

Herdewijn, Piet 2012-08-06T18:46:41Z Herman, Jean Gao, Ling-Jie Jonghe, Steven De Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents Cuveliers, Eva eng Jonghe, Steven De Calleja, Agnes Cuveliers, Eva Sienaert, Ilse Marchand, Arnaud deposit-license Lin, Yuan Waer, Mark Waer, Mark Marchand, Arnaud Clydesdale, Gavin 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 activity as measured in the Tumor Necrosis Factor (TNF) assay. Herman, Jean Pfleiderer, Wolfgang Publ. in: Bioorganic & medicinal chemistry letters ; 21 (2011), 1. - pp. 145-149 2011-01-01 Sefrioui, Hassane Calleja, Agnes 2012-08-06T18:46:41Z Clydesdale, Gavin Pfleiderer, Wolfgang Sienaert, Ilse Gao, Ling-Jie Lin, Yuan Herdewijn, Piet Sefrioui, Hassane

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