Title: Synthesis, immunosuppressive activity and structure-activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues
Authors: Jang, Mi-Yeon
De Jonghe, Steven
Van Belle, Kristien
Louat, Thierry
Waer, Mark
Herdewijn, Piet # ×
Issue Date: Feb-2010
Publisher: Pergamon-elsevier science ltd
Series Title: Bioorganic & medicinal chemistry letters vol:20 issue:3 pages:844-847
Abstract: 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. (C) 2010 Elsevier Ltd. All rights reserved.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Interface Valorization Platform (IVAP) (-)
Laboratory of Experimental Transplantation
× corresponding author
# (joint) last author

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