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Bioorg Med Chem. 2013 Mar 1;21(5):1209-18. doi: 10.1016/j.bmc.2012.12.032. Epub 2013 Jan 4.

Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay.

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1
KU Leuven, Interface Valorisation Platform, Kapucijnenvoer 33, 3000 Leuven, Belgium.

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 1.6 μM in the MLR assay.

PMID:
23347804
DOI:
10.1016/j.bmc.2012.12.032
[Indexed for MEDLINE]
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