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

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

  • Bioorg Med Chem Lett. 2010 Feb 1;20(3):844-7. doi: 10.1016/j.bmcl.2009.12.098.
Mi-Yeon Jang 1,  Steven De Jonghe,  Kristien Van Belle,  Thierry Louat,  Mark Waer,  Piet Herdewijn
Affiliations

Affiliation

  • 1 Catholic University of Leuven, Rega Institute, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
PMID: 20064721 DOI: 10.1016/j.bmcl.2009.12.098
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.

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