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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
Source :
Bioorganic & Medicinal Chemistry. Mar2013, Vol. 21 Issue 5, p1209-1218. 10p.
Publication Year :
2013

Abstract

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 IC50 value of 1.6μM in the MLR assay. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
09680896
Volume :
21
Issue :
5
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
85619145
Full Text :
https://doi.org/10.1016/j.bmc.2012.12.032