Title: Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay
Authors: Stella, Alessandro
Van Belle, Kristien
De Jonghe, Steven
Louat, Thierry
Herman, Jean
Rozenski, Jef
Waer, Mark
Herdewijn, Piet # ×
Issue Date: Mar-2013
Publisher: Pergamon
Series Title: Bioorganic & medicinal chemistry vol:21 issue:5 pages:1209-18
Article number: S0968-0896(12)01005-X
Abstract: A series of novel pyrimidine analogues were synthesized and evaluated for immunosuppressive activity in the Mixed Lymphocyte Reaction assay, which is well-known as the in vitro model for in vivo rejection after organ transplantation. Systematic variation of the substituents at positions 2, 4 and 6 of the pyrimidine scaffold led to the discovery of 2-benzylthio-5-cyano-6-(4-methoxyphenyl)-4-morpholinopyrimidine with an IC(50) value of 1.6μM in the MLR assay.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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