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Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics: synthesis and biological evaluation

Abstract : A series of seventeen beta-hydroxyphosphonate ribonucleoside analogues containing 4-substituted-1,2,3-triazoles was synthesized and fully characterized. Such compounds were designed as potential inhibitors of the cytosolic 5'-nucleotidase II (cN-II), an enzyme involved in the regulation of purine nucleotide pools. NMR and molecular modelling studies showed that a few derivatives adopted similar structural features to IMP or GMP. Five derivatives were identified as modest inhibitors with 53 to 64% of cN-II inhibition at 1 mM
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https://hal.archives-ouvertes.fr/hal-01812668
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Submitted on : Monday, July 6, 2020 - 3:24:56 PM
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Tai Nguyen Van, Audrey Hospital, Corinne Lionne, Lars P. Jordheim, Charles Dumontet, et al.. Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics: synthesis and biological evaluation. Beilstein Journal of Organic Chemistry, Beilstein-Institut, 2016, 12, pp.1476--1486. ⟨10.3762/bjoc.12.144⟩. ⟨hal-01812668⟩

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