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 triazole ring and the amide group. The synthesis presents a copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step with the solo obtainment of the anti-(1,4)-triazole derivatives. One of the obtained compounds showed a noteworthy general activity comparable to Imatinib and in particular it resulted more effective in reducing the fundamental function of cdc25A phosphatases in K-562 cell line.
N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl / F. Arioli, S. Borrelli, F. Colombo, F. Falchi, I. Filippi, E. Crespan, A. Naldini, G. Scalia, A. Silvani, G. Maga, F. Carraro, M. Botta, D. Passarella. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 6:11(2011), pp. 2009-2018.
N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl
A. Silvani;D. Passarella
2011
Abstract
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 triazole ring and the amide group. The synthesis presents a copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step with the solo obtainment of the anti-(1,4)-triazole derivatives. One of the obtained compounds showed a noteworthy general activity comparable to Imatinib and in particular it resulted more effective in reducing the fundamental function of cdc25A phosphatases in K-562 cell line.Pubblicazioni consigliate
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