Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.


Journal

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
ISSN: 1879-0720
Titre abrégé: Eur J Pharm Sci
Pays: Netherlands
ID NLM: 9317982

Informations de publication

Date de publication:
01 Nov 2020
Historique:
received: 05 06 2020
revised: 24 07 2020
accepted: 10 08 2020
pubmed: 18 8 2020
medline: 27 5 2021
entrez: 18 8 2020
Statut: ppublish

Résumé

Cancer is a heterogeneous disease, and its treatment requires the identification of new ways to thwart tumor cells. Amongst such emerging targets are glucose transporters (GLUTs, SLC2 family), which are overexpressed by almost all types of cancer cells; their inhibition provides a strategy to disrupt tumor metabolism selectively, leading to antitumor effects. Here, novel thiazolidinedione (TZD) derivatives were designed, synthesized, characterized, and evaluated for their GLUT1, GLUT4, and GLUT5 inhibitory potential, followed by in-vitro cytotoxicity determination in leukemic cell lines. Compounds G5, G16, and G17 inhibited GLUT1, with IC

Identifiants

pubmed: 32801003
pii: S0928-0987(20)30300-6
doi: 10.1016/j.ejps.2020.105512
pmc: PMC9398548
mid: NIHMS1622887
pii:
doi:

Substances chimiques

Glucose Transport Proteins, Facilitative 0
Glucose Transporter Type 1 0
Hypoglycemic Agents 0
Thiazolidinediones 0
2,4-thiazolidinedione AA68LXK93C

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

105512

Subventions

Organisme : NIGMS NIH HHS
ID : R01 GM123103
Pays : United States

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare no competing interests.

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Auteurs

Kalpana Tilekar (K)

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, Maharashtra, India.

Neha Upadhyay (N)

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, Maharashtra, India.

Markus Schweipert (M)

Department of Chemical Engineering and Biotechnology, University of Applied Sciences Darmstadt, Germany.

Jessica D Hess (JD)

The Cytometry, Screening and Imaging Core Facility & Border Biomedical Research Center & Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.

Lucasantiago Henze Macias (LH)

The Cytometry, Screening and Imaging Core Facility & Border Biomedical Research Center & Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.

Piotr Mrowka (P)

Department of Biophysics and Human Physiology, Medical University of Warsaw, Chalubinskiego, Warsaw, Poland.

Franz-Josef Meyer-Almes (FJ)

Department of Chemical Engineering and Biotechnology, University of Applied Sciences Darmstadt, Germany.

Renato J Aguilera (RJ)

The Cytometry, Screening and Imaging Core Facility & Border Biomedical Research Center & Department of Biological Sciences, The University of Texas at El Paso, El Paso, Texas, USA.

Cristina V Iancu (CV)

East Carolina Diabetes and Obesity Institute, Department of Chemistry, East Carolina University, Greenville, North Carolina, USA.

Jun-Yong Choe (JY)

East Carolina Diabetes and Obesity Institute, Department of Chemistry, East Carolina University, Greenville, North Carolina, USA; Department of Biochemistry and Molecular Biology, The Chicago Medical School, Rosalind Franklin University of Medicine and Science, North Chicago, Illinois, USA. Electronic address: choej18@ecu.edu.

C S Ramaa (CS)

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, Maharashtra, India. Electronic address: sinharamaa@yahoo.in.

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Classifications MeSH