Synthesis, immunosuppressive activity and structure–activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues
| Autor: | Mark Waer, Mi-Yeon Jang, Steven De Jonghe, Piet Herdewijn, Thierry Louat, Kristien Van Belle |
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| Rok vydání: | 2010 |
| Předmět: |
Chemistry
Stereochemistry Organic Chemistry Clinical Biochemistry Dose-Response Relationship Immunologic Pharmaceutical Science Mixed lymphocyte reaction Biochemistry Chemical synthesis Piperazines In vitro Structure-Activity Relationship Pyrimidine analogue Pyrimidines Drug Discovery Humans Molecular Medicine Structure–activity relationship Lymphocytes Lymphocyte Culture Test Mixed Molecular Biology Immunosuppressive Agents |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:844-847 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2009.12.098 |
| Popis: | The synthesis of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidines is described. The synthetic route allows introducing structural variety at positions 2, 4 and 6 of the scaffold. Evaluation of their immunosuppressive activity in a Mixed Lymphocyte Reaction (MLR) assay revealed that the most potent compound has an IC50-value of 66 nM and therefore deserves attention for further medicinal chemistry optimization. |
| Databáze: | OpenAIRE |
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