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

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 mos...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (3), p.844-847
Hauptverfasser:	Jang, Mi-Yeon, Jonghe, Steven De, Belle, Kristien Van, Louat, Thierry, Waer, Mark, Herdewijn, Piet
Format:	Artikel
Sprache:	eng
Schlagworte:	Dose-Response Relationship, Immunologic Humans Immunosuppressive activity Immunosuppressive Agents - chemical synthesis Immunosuppressive Agents - pharmacology Lymphocyte Culture Test, Mixed - methods Lymphocytes - drug effects Lymphocytes - immunology Medicinal chemistry MLR assay Piperazines - chemical synthesis Piperazines - pharmacology Pyrimidines - chemical synthesis Pyrimidines - pharmacology Structure-Activity Relationship Thieno[2,3- d]pyrimidine
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.12.098