Title: Synthesis and in vitro evaluation of 2-amino-4-N-piperazinyl-6-(3,4-dimethoxyphenyl)-pteridines as dual immunosuppressive and anti-inflammatory agents
Authors: 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 # ×
Issue Date: Jan-2011
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:21 issue:1 pages:145-149
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 IC(50) 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.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Laboratory of Experimental Transplantation
Interface Valorization Platform (IVAP) (-)
Department of Experimental Medicine (-)
× corresponding author
# (joint) last author

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