Evidence map›Paper›PMID 34873879›Full record

ArticleFEBS open bio2022

4,5,7-Trisubstituted indeno[1,2-b]indole inhibits CK2 activity in tumor cells equivalent to CX-4945 and shows strong anti-migratory effects.

Robin Birus, Ehab El-Awaad, Laurens Ballentin, Faten Alchab, Dagmar Aichele, Laurent Ettouati, Claudia Götz, Marc Le Borgne, Joachim Jose

Open access · goldAbstract read
In one paragraph

Article in FEBS open bio, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.2field-weighted citation impact, top 46% 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

4 citing papers in PubMed, 6 citations in OpenAlex.

  1. Article
  2. Article
  3. Preparation and antimicrobial activity of Mono-, Bis, and Tris-4,9-Dihydroxy-7,7-Dimethyl-5-(mono-substituted-aryl)-Hexahydro-Indeno[1,2-b]Indole-9,10-Dione derivatives.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Article
  4. 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

9 authors at 3 institutions in 3 countries.

Robin BirusInstitute of Pharmaceutical and Medicinal Chemistry, Westfälische Wilhelms-Universtität Münster, Germany.ORCID 0000-0002-9543-3954
Ehab El-AwaadInstitute of Pharmaceutical and Medicinal Chemistry, Westfälische Wilhelms-Universtität Münster, Germany.ORCID 0000-0003-3383-6384
Laurens BallentinInstitute of Pharmaceutical and Medicinal Chemistry, Westfälische Wilhelms-Universtität Münster, Germany.
Faten AlchabEEA 4446 Bioactive Molecules and Medicinal Chemistry, Faculté de Pharmacie-ISPB, SFR Santé Lyon-Est CNRS UMS3453-INSERM US7, Université Claude Bernard Lyon 1, Université de Lyon, France.ORCID 0000-0003-2123-655X
Dagmar AicheleInstitute of Pharmaceutical and Medicinal Chemistry, Westfälische Wilhelms-Universtität Münster, Germany.ORCID 0000-0001-5937-0450
Laurent EttouatiCNRS UMR 5246 Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), Faculté de Pharmacie, ISPB, Université Lyon 1, Université de Lyon, France.ORCID 0000-0002-2150-2734
Claudia GötzMedical Biochemistry and Molecular Biology, Saarland University, Germany.
Marc Le BorgneSmall Molecules for Biological Targets Team, Centre de recherche en cancérologie de Lyon, Centre Léon Bérard, CNRS 5286, INSERM 1052, Université Claude Bernard Lyon 1, Université de Lyon, France.ORCID 0000-0003-1398-075X
Joachim JoseInstitute of Pharmaceutical and Medicinal Chemistry, Westfälische Wilhelms-Universtität Münster, Germany.ORCID 0000-0002-0666-2676
University of Münster · DEUniversité Claude Bernard Lyon 1 · FRSaarland University · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Highly pleiotropic and constitutively active protein kinase CK2 is a key target in cancer therapy, but only one small-molecule inhibitor has reached clinical trials-CX-4945. In this study, we present the indeno[1,2-b]indole derivative 5-isopropyl-4-methoxy-7-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione (5a-2) that decreased the intracellular CK2 activity in A431, A549, and LNCaP tumor cell lines analogous to CX-4945 (> 75% inhibition at 20 µm) and similarly blocked CK2-specific Akt phosphorylation in LNCaP cells. Cellular uptake analysis demonstrated higher intracellular concentrations of 5a-2 (408.3 nm) compared with CX-4945 (119.3 nm). This finding clarifies the comparable effects of both compounds on the intracellular CK2 activity despite their different inhibitory potency in vitro [IC

Indexed as

Casein Kinase IINaphthyridinesIndolesPhenazinesCasein Kinase IIIndolesNaphthyridinesPhenazinessilmitasertibCK2HPLC-MS/MSindeno[1,2-b]indolelive-cell imagingpharmacokinetics

Identifiers

PMID34873879
PMCPMC8804612
OpenAlexW4200053739

What OpenQuestion holds

Textmetadata
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.