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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

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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

Type of Publication: Journal article
Author: Jonghe, Steven De; 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
Year of publication: 2011
Published in: Bioorganic & Medicinal Chemistry Letters ; 21 (2011), 1. - pp. 145-149. - ISSN 0960-894X. - eISSN 1464-3405
Pubmed ID: 21131199
DOI (citable link): https://dx.doi.org/10.1016/j.bmcl.2010.11.053
Summary:
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.
Subject (DDC): 540 Chemistry
Keywords: pteridine, immunosuppressive drugs, anti-inflammatory drugs

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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} }

terms-of-use 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 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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