Evidence map›Paper›PMID 32298535›Full record

ArticleChemMedChem2020

Synthesis and Characterization of Telmisartan-Derived Cell Death Modulators to Circumvent Imatinib Resistance in Chronic Myeloid Leukemia.

Anna M Schoepf, Stefan Salcher, Verena Hohn, Florina Veider, Petra Obexer, Ronald Gust

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 30% 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

5 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Reaction Behavior of [1,3-Diethyl-4,5-diphenyl-1Journal of medicinal chemistry · 2023
    Article
  3. Review
  4. Article
  5. 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

6 authors at 2 institutions in 1 country.

Anna M SchoepfDepartment of Pharmaceutical Chemistry Institute of Pharmacy CMBI - Center for Molecular Biosciences Innsbruck, University of Innsbruck, CCB - Centrum for Chemistry and Biomedicine, Innrain 80/82, 6020, Innsbruck, Austria.
Stefan SalcherTyrolean Cancer Research Institute, Innrain 66, 6020, Innsbruck, Austria.
Verena HohnDepartment of Pharmaceutical Chemistry Institute of Pharmacy CMBI - Center for Molecular Biosciences Innsbruck, University of Innsbruck, CCB - Centrum for Chemistry and Biomedicine, Innrain 80/82, 6020, Innsbruck, Austria.
Florina VeiderDepartment of Pharmaceutical Chemistry Institute of Pharmacy CMBI - Center for Molecular Biosciences Innsbruck, University of Innsbruck, CCB - Centrum for Chemistry and Biomedicine, Innrain 80/82, 6020, Innsbruck, Austria.
Petra ObexerTyrolean Cancer Research Institute, Innrain 66, 6020, Innsbruck, Austria.
Ronald GustDepartment of Pharmaceutical Chemistry Institute of Pharmacy CMBI - Center for Molecular Biosciences Innsbruck, University of Innsbruck, CCB - Centrum for Chemistry and Biomedicine, Innrain 80/82, 6020, Innsbruck, Austria.ORCID 0000-0002-0427-4012
Universität Innsbruck · ATInnsbruck Medical University · AT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

New strategies to eradicate cancer stem cells in chronic myeloid leukemia (CML) include a combination of imatinib with peroxisome proliferator-activated receptor gamma (PPARγ) ligands. Recently, we identified the partial PPARγ agonist telmisartan as effective sensitizer of resistant K562 CML cells to imatinib treatment. Here, the importance of the heterocyclic core on the cell death-modulating effects of the telmisartan-derived lead 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid (3 b) was investigated. Inspired by the pharmacodynamics of HYL-6d and the selective PPARγ ligand VSP-51, the benzimidazole was replaced by a carbazole or an indole core. The results indicate no correlation between PPARγ activation and sensitization of resistant CML cells to imatinib. The 2-COOH derivatives of the carbazoles or indoles achieved low activity at PPARγ, while the benzimidazoles showed 60-100 % activation. Among the 2-CO

Indexed as

AnimalsCarbazolesCell DeathChlorocebus aethiopsCOS CellsDrug Resistance, NeoplasmHumansImatinib MesylateIndolesK562 CellsLeukemia, Myelogenous, Chronic, BCR-ABL PositiveMolecular StructurePPAR gammaStructure-Activity RelationshipTelmisartanCarbazolesImatinib MesylateIndolesPPAR gammaTelmisartanchronic myeloid leukemiaimatinib resistanceperoxisome proliferator-activated receptor gammasensitizersstructure-activity relationship

Identifiers

PMID32298535
PMCPMC7318623
OpenAlexW3016764526

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.