Evidence map›Paper›PMID 34536671›Full record

ArticleEuropean journal of medicinal chemistry2021

Anti-schistosomal activities of quinoxaline-containing compounds: From hit identification to lead optimisation.

Gilda Padalino, Nelly El-Sakkary, Lawrence J Liu, Chenxi Liu, Danielle S G Harte, Rachel E Barnes, Edward Sayers, Josephine Forde-Thomas, Helen Whiteland, Marcella Bassetto and 7 more

Open access · hybridAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
2.8field-weighted citation impact, top 10% 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

10 citing papers in PubMed, 23 citations in OpenAlex.

  1. Article
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  7. Small Molecule Ligands of the BET-like Bromodomain,Journal of medicinal chemistry · 2023
    Article
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  9. 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

17 authors at 4 institutions in 2 countries.

Gilda PadalinoInstitute of Biological, Environmental and Rural Sciences (IBERS), Aberystwyth University, Aberystwyth, SY23 3DA, United Kingdom.
Nelly El-SakkaryCenter for Discovery and Innovation in Parasitic Diseases (CDIPD), Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Lawrence J LiuCenter for Discovery and Innovation in Parasitic Diseases (CDIPD), Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Chenxi LiuCenter for Discovery and Innovation in Parasitic Diseases (CDIPD), Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Danielle S G HarteSwansea University Medical School, Swansea University, Swansea, SA2 8PP, United Kingdom.
Rachel E BarnesSwansea University Medical School, Swansea University, Swansea, SA2 8PP, United Kingdom.
Edward SayersSchool of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, United Kingdom.
Josephine Forde-ThomasInstitute of Biological, Environmental and Rural Sciences (IBERS), Aberystwyth University, Aberystwyth, SY23 3DA, United Kingdom.
Helen WhitelandInstitute of Biological, Environmental and Rural Sciences (IBERS), Aberystwyth University, Aberystwyth, SY23 3DA, United Kingdom.
Marcella BassettoDepartment of Chemistry, College of Science and Engineering, Swansea University, Swansea, SA2 8PP, United Kingdom.
Salvatore FerlaSwansea University Medical School, Swansea University, Swansea, SA2 8PP, United Kingdom.
George JohnsonSwansea University Medical School, Swansea University, Swansea, SA2 8PP, United Kingdom.
Arwyn T JonesSchool of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, United Kingdom.
Conor R CaffreyCenter for Discovery and Innovation in Parasitic Diseases (CDIPD), Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Iain ChalmersInstitute of Biological, Environmental and Rural Sciences (IBERS), Aberystwyth University, Aberystwyth, SY23 3DA, United Kingdom.
Andrea BrancaleSchool of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, United Kingdom.
Karl F HoffmannInstitute of Biological, Environmental and Rural Sciences (IBERS), Aberystwyth University, Aberystwyth, SY23 3DA, United Kingdom. Electronic address: krh@aber.ac.uk.
Aberystwyth University · GBSwansea University · GBUniversity of California San Diego · USCardiff University · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Schistosomiasis is a neglected disease of poverty that is caused by infection with blood fluke species contained within the genus Schistosoma. For the last 40 years, control of schistosomiasis in endemic regions has predominantly been facilitated by administration of a single drug, praziquantel. Due to limitations in this mono-chemotherapeutic approach for sustaining schistosomiasis control into the future, alternative anti-schistosomal compounds are increasingly being sought by the drug discovery community. Herein, we describe a multi-pronged, integrated strategy that led to the identification and further exploration of the quinoxaline core as a promising anti-schistosomal scaffold. Firstly, phenotypic screening of commercially available small molecules resulted in the identification of a moderately active hit compound against Schistosoma mansoni (1, EC

Indexed as

AnimalsCell Line, TumorCell SurvivalDose-Response Relationship, DrugHumansMolecular StructureQuinoxalinesSchistosoma haematobiumSchistosoma japonicumSchistosoma mansoniSchistosomiasis mansoniStructure-Activity RelationshipQuinoxalinesDrug discoveryQuinoxalineSARSchistosomiasis

Identifiers

PMID34536671
PMCPMC8626775
OpenAlexW3199320318

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.