N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl. (Articolo in rivista)

Type
Label
  • N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl. (Articolo in rivista) (literal)
Anno
  • 2011-01-01T00:00:00+01:00 (literal)
Alternative label
  • Arioli F, Borrelli S, Colombo F, Falchi F, Filippi I, Crespan E, Naldini A, Scalia G, Silvani A, Maga G, Carraro F, Botta M, Passarella D. (2011)
    N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl.
    in ChemMedChem (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Arioli F, Borrelli S, Colombo F, Falchi F, Filippi I, Crespan E, Naldini A, Scalia G, Silvani A, Maga G, Carraro F, Botta M, Passarella D. (literal)
Pagina inizio
  • 2009 (literal)
Pagina fine
  • 2018 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 6 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • [a] Dr. F. Arioli, Dr. S. Borrelli, Dr. F. Colombo, Dr. A. Silvani, Prof. Dr. D. Passarella Dipartimento di Chimica Organica e Industriale Universit? degli Studi di Milan Via G. Venezian 21, 20133 Milano (Italy) E-mail: daniele.passarella@unimi.it [b] Dr. F. Falchi, Prof. Dr. M. Botta Dipartimento Farmaco Chimico Tecnologico Universit? degli Studi di Siena, Via A. Moro, 53100 Siena (Italy) [c] Dr. I. Filippi, Dr. A. Naldini, Dr. G. Scalia, Prof. Dr. F. Carraro Dipartimento di Fisiologia Universit? degli Studi di Siena, Via A. Moro, 53100 Siena (Italy) [d] Dr. E. Crespan, Dr. G. Maga Istituto di Genetica Molecolare IGM-CNR Via Abbiategrasso 207, 27100 Pavia (Italy) (literal)
Titolo
  • N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl. (literal)
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 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. (literal)
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