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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2011
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Jonghe, Steven De
Marchand, Arnaud
Gao, Ling-Jie
Calleja, Agnes
Cuveliers, Eva
Sienaert, Ilse
Herman, Jean
Clydesdale, Gavin
Sefrioui, Hassane
Lin, Yuan
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Bioorganic & Medicinal Chemistry Letters. 2011, 21(1), pp. 145-149. ISSN 0960-894X. eISSN 1464-3405. Available under: doi: 10.1016/j.bmcl.2010.11.053
Zusammenfassung

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.

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540 Chemie
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pteridine, immunosuppressive drugs, anti-inflammatory drugs
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ISO 690JONGHE, 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. 2011, 21(1), pp. 145-149. ISSN 0960-894X. eISSN 1464-3405. Available under: doi: 10.1016/j.bmcl.2010.11.053
BibTex
@article{Jonghe2011-01-01Synth-19906,
  year={2011},
  doi={10.1016/j.bmcl.2010.11.053},
  title={Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents},
  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}
}
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