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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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| 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 |
| Institution: | a 4AZA Bioscience, Kapucijnenvoer 33, 3000 Leuven, Belgium b Fachbereich Chemie, Universität Konstanz, Postfach 5560, 78457 Konstanz, Germany c Laboratory of Experimental Transplantation, Katholieke Universiteit Leuven, Campus Gasthuisberg, Herestraat 49, 3000 Leuven, Belgium d Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium |
| 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 activity as measured in the Tumor Necrosis Factor (TNF) assay. |
| Keywords: | Pteridine Immunosuppressive drugs Anti-inflammatory drugs |
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