Evidence map›Paper›PMID 32446120›Full record

ArticleBioorganic chemistry2020

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation.

Neha Upadhyay, Kalpana Tilekar, Niklas Jänsch, Markus Schweipert, Jessica D Hess, Luca Henze Macias, Piotr Mrowka, Renato J Aguilera, Jun-Yong Choe, Franz-Josef Meyer-Almes and 1 more

Open access · greenAbstract read
In one paragraph

Article in Bioorganic chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
2.8field-weighted citation impact, top 8% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 48 citations in OpenAlex.

  1. Review
  2. Direct targeting of GLUT1 in cancer: A decade of inhibitor discovery and medicinal chemistry insights.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Review
  3. Review
  4. Review
  5. Discovery and Characterization of Novel Non-Hydroxamate HDAC11 Inhibitors.International journal of molecular sciences · 2025
    Article
  6. Review
  7. Review
  8. Article
  9. Review
  10. Review
  11. Article
  12. Review
  13. Article
  14. Permuted 2,4-thiazolidinedione (TZD) analogs as GLUT inhibitors and their in-vitro evaluation in leukemic cells.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2020
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors at 4 institutions in 3 countries.

Neha UpadhyayDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, India.
Kalpana TilekarDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, India.
Niklas JänschDepartment of Chemical Engineering and Biotechnology, University of Applied Science, Darmstadt, Germany.
Markus SchweipertDepartment of Chemical Engineering and Biotechnology, University of Applied Science, Darmstadt, Germany.
Jessica D HessThe Cellular Characterization and Biorepository Core Facility & Border Biomedical Research Centre & Department of Biological Sciences, The University of Texas at El Paso, El Paso, TX, USA.
Luca Henze MaciasThe Cellular Characterization and Biorepository Core Facility & Border Biomedical Research Centre & Department of Biological Sciences, The University of Texas at El Paso, El Paso, TX, USA.
Piotr MrowkaDepartment of Biophysics and Human Physiology, Medical University of Warsaw, Chalubinskiego, Warsaw, Poland; Institute of Hematology and Blood Transfusion, Indira Gandhi St., Warsaw, Poland.
Renato J AguileraThe Cellular Characterization and Biorepository Core Facility & Border Biomedical Research Centre & Department of Biological Sciences, The University of Texas at El Paso, El Paso, TX, USA.
Jun-Yong ChoeEast Carolina Diabetes and Obesity Institute, East Carolina University, Greenville, NC 27834, USA; Department of Biochemistry and Molecular Biology, The Chicago Medical School, Rosalind Franklin University of Medicine and Science, North Chicago, IL, USA.
Franz-Josef Meyer-AlmesDepartment of Chemical Engineering and Biotechnology, University of Applied Science, Darmstadt, Germany. Electronic address: franz-josef.meyer-almes@h-da.de.
C S RamaaDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi Mumbai, India. Electronic address: sinharamaa@yahoo.in.
Bharati Vidyapeeth Deemed University · INThe University of Texas at El Paso · USEast Carolina University · USMedical University of Warsaw · PL

Funding

UTEP Border Biomedical Research CenterU54MD007592 · NIMHD · UNIVERSITY OF TEXAS EL PASO · PI Gabriel Andrew Frietze · 2019 to 2026
$35.1M
NIMHD NIH HHS U54 MD007592
6 · The paper itself

Abstract

Epigenetics plays a fundamental role in cancer progression, and developing agents that regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs, HDAC8 is one of the essential epigenetic players in cancer progression. Therefore, we designed, synthesized, purified, and structurally characterized novel compounds containing N-substituted TZD (P1-P25). Cell viability assay of all compounds on leukemic cell lines (CEM, K562, and KCL22) showed the cytotoxic potential of P8, P9, P10, P12, P19, and P25. In-vitro screening of different HDACs isoforms revealed that P19 was the most potent and selective inhibitor for HDAC8 (IC

Indexed as

ApoptosisBinding SitesCell LineCell SurvivalDrug Evaluation, PreclinicalGlucose Transporter Type 1Histone Deacetylase InhibitorsHistone DeacetylasesHumansMolecular Docking SimulationProtein IsoformsRepressor ProteinsStructure-Activity RelationshipThiazolidinedionesGlucose Transporter Type 1HDAC8 protein, humanHistone Deacetylase InhibitorsHistone DeacetylasesProtein IsoformsRepressor ProteinsThiazolidinedionesDockingGLUTHDACLeukemiaN-substituted thiazolidinediones

Identifiers

PMID32446120
PMCPMC7302971
OpenAlexW3024956451

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.