title: 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 β-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.
authors: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS - Université de Montpellier - ENSCM, Campus Triolet, cc1705, Place Eugène Bataillon, 34095 Montpellier, France.
authors: Tai
authors: T
authors: Nguyen Van
authors: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS - Université de Montpellier - ENSCM, Campus Triolet, cc1705, Place Eugène Bataillon, 34095 Montpellier, France.
authors: Audrey
authors: A
authors: Hospital
authors: Centre d'études d'agents Pathogènes et Biotechnologies pour la Santé (CPBS), FRE 3689 CNRS - Université de Montpellier, 1919 route de Mende, 34293 Montpellier, France.
authors: Corinne
authors: C
authors: Lionne
authors: Université de Lyon, Université Claude Bernard Lyon 1, INSERM 1052, CNRS 5286, Centre Léon Bérard, Centre de Recherche en Cancérologie de Lyon, 69008 Lyon, France.
authors: Lars P
authors: LP
authors: Jordheim
authors: Université de Lyon, Université Claude Bernard Lyon 1, INSERM 1052, CNRS 5286, Centre Léon Bérard, Centre de Recherche en Cancérologie de Lyon, 69008 Lyon, France.
authors: Charles
authors: C
authors: Dumontet
authors: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS - Université de Montpellier - ENSCM, Campus Triolet, cc1705, Place Eugène Bataillon, 34095 Montpellier, France.
authors: Christian
authors: C
authors: Périgaud
authors: Centre d'études d'agents Pathogènes et Biotechnologies pour la Santé (CPBS), FRE 3689 CNRS - Université de Montpellier, 1919 route de Mende, 34293 Montpellier, France.
authors: Laurent
authors: L
authors: Chaloin
authors: Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS - Université de Montpellier - ENSCM, Campus Triolet, cc1705, Place Eugène Bataillon, 34095 Montpellier, France.
authors: Suzanne
authors: S
authors: Peyrottes
keywords: cN-II inhibitors; cancer; nucleotide; phosphonate; triazole