2. Academic Validation
  3. 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

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

  • J Med Chem. 2017 Feb 23;60(4):1523-1533. doi: 10.1021/acs.jmedchem.6b01803.
Hella Amdouni 1,  Guillaume Robert 2,  Mohsine Driowya 1 3,  Nathan Furstoss 2,  Camille Métier 1,  Alix Dubois 2,  Maeva Dufies 2,  Marwa Zerhouni 2,  François Orange 4,  Sandra Lacas-Gervais 4,  Khalid Bougrin 3,  Anthony R Martin 1,  Patrick Auberger 2,  Rachid Benhida 1
Affiliations

Affiliations

  • 1 Institut de Chimie de Nice UMR7272, Université Côte d'Azur, CNRS , 06108 Nice, France.
  • 2 Centre Méditerranéen de Médecine Moléculaire, Université Côte d'Azur, UMR INSERM U1065 , 06204 Nice, France.
  • 3 Laboratoire de Chimie des Plantes et de Synthèse Organique et Bioorganique, URAC23, Faculté des Sciences, Université Mohammed V , B.P. 1014, Rabat, Morocco.
  • 4 Centre Commun de Microscopie Appliquée , 06108 Nice, France.
PMID: 28094938 DOI: 10.1021/acs.jmedchem.6b01803
Abstract

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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z