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N-[2-Methyl-5-(triazol-1-yl)phenyl]pyrimidin-2-amine as a Scaffold for the Synthesis of Inhibitors of Bcr-Abl.
MedLine Citation:
PMID:  21990039     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Federica Arioli; Stella Borrelli; Francesco Colombo; Federico Falchi; Irene Filippi; Emmanuele Crespan; Antonella Naldini; Giusy Scalia; Alessandra Silvani; Giovanni Maga; Fabio Carraro; Maurizio Botta; Daniele Passarella
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-8-30
Journal Detail:
Title:  ChemMedChem     Volume:  -     ISSN:  1860-7187     ISO Abbreviation:  -     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-10-12     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101259013     Medline TA:  ChemMedChem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Affiliation:
Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milan, Via G. Venezian 21, 20133 Milano (Italy).
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