Evidence map›Paper›PMID 32403277›Full record

ArticleMolecules (Basel, Switzerland)2020

Search for ABCB1 Modulators Among 2-Amine-5-Arylideneimidazolones as a New Perspective to Overcome Cancer Multidrug Resistance.

Aneta Kaczor, Márta Nové, Annamária Kincses, Gabriella Spengler, Ewa Szymańska, Gniewomir Latacz, Jadwiga Handzlik

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 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
0.8field-weighted citation impact, top 25% 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, 19 citations in OpenAlex.

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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

7 authors at 2 institutions in 2 countries.

Aneta KaczorDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.ORCID 0000-0001-9899-1794
Márta NovéDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, Hungary.
Annamária KincsesDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, Hungary.
Gabriella SpenglerDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, Hungary.ORCID 0000-0002-4499-388X
Ewa SzymańskaDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.ORCID 0000-0003-3025-7002
Gniewomir LataczDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.ORCID 0000-0001-9247-2598
Jadwiga HandzlikDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.ORCID 0000-0002-3674-3581
Jagiellonian University · PLUniversity of Szeged · HU

Funding

Hungarian Grant EFOP 3.6.3-VEKOP-16-2017-00009Ministerstwo Nauki i Szkolnictwa Wyższego "Diamond Grant" no 0169/DIA/2017/46Uniwersytet Jagielloński Collegium Medicum N42/DBS/000070 and N42/DBS/000027
6 · The paper itself

Abstract

Multidrug resistance (MDR) is a severe problem in the treatment of cancer with overexpression of glycoprotein P (Pgp, ABCB1) as a reason for chemotherapy failure. A series of 14 novel 5-arylideneimidazolone derivatives containing the morpholine moiety, with respect to two different topologies (groups A and B), were designed and obtained in a three- or four-step synthesis, involving the Dimroth rearrangement. The new compounds were tested for their inhibition of the ABCB1 efflux pump in both sensitive (parental (PAR)) and ABCB1-overexpressing (MDR) T-lymphoma cancer cells in a rhodamine 123 accumulation assay. Their cytotoxic and antiproliferative effects were investigated by a thiazolyl blue tetrazolium bromide (MTT) assay. For active compounds, an insight into the mechanisms of action using either the luminescent Pgp-Glo™ Assay in vitro or docking studies to human Pgp was performed. The safety profile in vitro was examined. Structure-activity relationship (SAR) analysis was discussed. The most active compounds, representing both 2-substituted- (

Indexed as

AnimalsAntineoplastic AgentsATP Binding Cassette Transporter, Subfamily BCell Line, TumorCell ProliferationCell SurvivalDoxorubicinDrug Resistance, MultipleDrug Resistance, NeoplasmHumansImidazolesInhibitory Concentration 50In Vitro TechniquesLymphoma, T-CellMiceModels, MolecularABCB1 protein, humanAntineoplastic AgentsATP Binding Cassette Transporter, Subfamily BDoxorubicinImidazolesimidazolonemorpholineMorpholinesRhodamine 123Verapamil5-arylideneimidazoloneABCB1 modulatorcancer MDRDimroth rearrangementPgpPgp dockingrhodamine 123 accumulation assayT-lymphoma cancer cell

Identifiers

PMID32403277
PMCPMC7249047
OpenAlexW3020842494

What OpenQuestion holds

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LicenceCC BY
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.