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J Med Chem. 2017 Feb 23;60(4):1523-1533. doi: 10.1021/acs.jmedchem.6b01803. Epub 2017 Feb 2.

In Vitro and in Vivo Evaluation of Fully Substituted (5-(3-Ethoxy-3-oxopropynyl)-4-(ethoxycarbonyl)-1,2,3-triazolyl-glycosides as Original Nucleoside Analogues to Circumvent Resistance in Myeloid Malignancies.

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Institut de Chimie de Nice UMR7272, Université Côte d'Azur, CNRS , 06108 Nice, France.
Centre Méditerranéen de Médecine Moléculaire, Université Côte d'Azur, UMR INSERM U1065 , 06204 Nice, France.
Laboratoire de Chimie des Plantes et de Synthèse Organique et Bioorganique, URAC23, Faculté des Sciences, Université Mohammed V , B.P. 1014, Rabat, Morocco.
Centre Commun de Microscopie Appliquée , 06108 Nice, France.


A series of nucleoside analogues bearing a 1,4,5-trisubstituted-1,2,3-triazole aglycone was synthesized using a straightforward click/electrophilic addition or click/oxidative coupling tandem procedures. SAR analysis, using cell culture assays, led to the discovery of a series of compounds belonging to the 5-alkynyl-1,2,3-triazole family that exhibits potent antileukemic effects on several hematologic malignancies including chronic myeloid leukemia (CML) and myelodysplastic syndromes (MDS) either sensitive or resistant to their respective therapy. Compound 4a also proved efficient in vivo on mice xenografted with SKM1-R MDS cell line. Additionally, some insights in its mode of action revealed that this compound induced cell death by caspase and autophagy induction.

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