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Title: N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a scaffold for the synthesis of inhibitors of Bcr-Abl.
Authors: Arioli, F
Borrelli, S
Colombo, F
Falchi, F
Filippi, Irene
Crespan, E
Naldini, Antonella
Scalia, Giusy
Silvani, A
Maga, G
Carraro, Fabio
Botta, Maurizio 
Passarella, D.
Issue Date: 2011
Project: None 
N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine derivatives were synthesized and evaluated in vitro for their potential use as inhibitors of Bcr-Abl. The design is based on the bioisosterism between the 1,2,3-triazole ring and the amide group. The synthesis involves a copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) as the key step, with the exclusive production of anti-(1,4)-triazole derivatives. One of the compounds obtained shows general activity similar to that of imatinib; in particular, it was observed to be more effective in decreasing the fundamental function of cdc25A phosphatases in the K-562 cell line.
ISSN: 1860-7187
DOI: 10.1002/cmdc.201100304
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