Evidence map›Paper›PMID 36284193›Full record

ArticleChemistryOpen2022

Synthesis and Anti-Inflammatory Activity of 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-Derived NRF2 Activators.

Kit-Kay Mak, Zhang Shiming, Ola Epemolu, Albena T Dinkova-Kostova, Geoffrey Wells, Irina G Gazaryan, Raghavendra Sakirolla, Zulkefeli Mohd, Mallikarjuna Rao Pichika

Abstract read
In one paragraph

Article in ChemistryOpen, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
–field-weighted citation impact
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

7 citing papers in PubMed.

  1. Article
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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

9 authors.

Kit-Kay MakPharmaceutical Chemistry Department, International Medical University, 126 Jalan Jalil Perkasa 19, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.ORCID 0000-0001-6939-5280
Zhang ShimingSchool of Postgraduate Studies, International Medical University, 126 Jalan Jalil Perkasa 19 Bukit Jalil, 57000, Kuala Lumpur, Malaysia.ORCID 0000-0003-1049-924X
Ola EpemoluPrincipal research scientist- in vitro/in vivo DMPK, Charles River Laboratories Edinburgh Ltd, Tranent, East Lothian, Scotland, UK.ORCID 0000-0001-7741-3928
Albena T Dinkova-KostovaSchool of Medicine, Jacqui Wood Cancer Centre, University of Dundee, Dundee, Scotland, UK.ORCID 0000-0003-0316-9859
Geoffrey WellsUCL School of Pharmacy, University College London, London, WC1N 1AX, UK.ORCID 0000-0002-0253-911X
Irina G GazaryanFaculty of Biology and Biotechnology, National Research University Higher School of Economics, Moscow, Russia.ORCID 0000-0002-9670-5579
Raghavendra SakirollaDepartment of Chemistry, Central University of Karnataka, Gulbarga, Karnataka, India.
Zulkefeli MohdPharmaceutical Chemistry Department, International Medical University, 126 Jalan Jalil Perkasa 19, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.
Mallikarjuna Rao PichikaPharmaceutical Chemistry Department, International Medical University, 126 Jalan Jalil Perkasa 19, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.ORCID 0000-0002-9761-8266

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

This is the first study investigating the nuclear factor (erythroid-derived 2)-like 2 (NRF2) activity of compounds containing a new scaffold, tetrahydrobenzo[b]thiophene. Eighteen compounds were synthesised and confirmed their NRF2 activation through NQO1 enzymatic activity and mRNA expression of NQO1 and HO-1 in Hepa-1c1c7 cells. The compounds disrupted the interaction between Kelch-like ECH-associated protein 1 (KEAP1) and NRF2 via interfering with the KEAP1's Kelch domain. The compounds exhibited anti-inflammatory activity in Escherichia coli Lipopolysaccharide (LPS

Indexed as

NF-E2-Related Factor 2NF-kappa BAnimalsAnti-Inflammatory AgentsCyclooxygenase 2CytokinesDinoprostoneHumansInflammation MediatorsInterleukin-6Kelch-Like ECH-Associated Protein 1LipopolysaccharidesMiceRatsRNA, MessengerThiophenesAnti-Inflammatory AgentsCyclooxygenase 2CytokinesDinoprostoneInflammation MediatorsInterleukin-6Kelch-Like ECH-Associated Protein 1LipopolysaccharidesNF-E2-Related Factor 2NF-kappa BRNA, MessengerThiophenesTumor Necrosis Factor-alphaanti-inflammatoryNRF2 activatorstetrahydrobenzothiophenethiophenes

Identifiers

PMID36284193
PMCPMC9596610

What OpenQuestion holds

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LicenceCC BY-NC
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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.