Synthesis, immunosuppressive activity and structure-activity relationship study of a new series of 4-N-piperazinyl-thieno[2,3-d]pyrimidine analogues

ArticleinBioorganic & medicinal chemistry letters 20(3):844-7 · February 2010with2 Reads
Impact Factor: 2.42 · DOI: 10.1016/j.bmcl.2009.12.098 · Source: PubMed

    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 IC(50)-value of 66 nM and therefore deserves attention for further medicinal chemistry optimization.