Evidence map›Paper›PMID 34251942›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2021

Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines.

Olga Cruz-López, Matilde Ner, Francho Nerín-Fonz, Yaiza Jiménez-Martínez, David Araripe, Juan A Marchal, Houria Boulaiz, Hugo Gutiérrez-de-Terán, Joaquín M Campos, Ana Conejo-García

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.1field-weighted citation impact, top 26% 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

6 citing papers in PubMed, 14 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

10 authors at 2 institutions in 4 countries.

Olga Cruz-LópezDepartment of Medicinal and Organic Chemistry, Faculty of Pharmacy, University of Granada, Granada, Spain.ORCID https://orcid.org/0000-0002-9807-4061
Matilde NerDepartment of Medicinal and Organic Chemistry, Faculty of Pharmacy, University of Granada, Granada, Spain.
Francho Nerín-FonzDepartment of Cell and Molecular Biology, Uppsala University, Uppsala, Sweeden.
Yaiza Jiménez-MartínezBiosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Granada, Spain.
David AraripeDepartment of Cell and Molecular Biology, Uppsala University, Uppsala, Sweeden.
Juan A MarchalBiosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Granada, Spain.ORCID https://orcid.org/0000-0002-4996-8261
Houria BoulaizBiosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Granada, Spain.ORCID https://orcid.org/0000-0003-4433-7556
Hugo Gutiérrez-de-TeránDepartment of Cell and Molecular Biology, Uppsala University, Uppsala, Sweeden.
Joaquín M CamposDepartment of Medicinal and Organic Chemistry, Faculty of Pharmacy, University of Granada, Granada, Spain.ORCID https://orcid.org/0000-0002-9035-8123
Ana Conejo-GarcíaDepartment of Medicinal and Organic Chemistry, Faculty of Pharmacy, University of Granada, Granada, Spain.ORCID https://orcid.org/0000-0001-5776-7315
Universidad de Granada · ESUppsala University · SE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A series of 11 new substituted 1,5-dihydro-4,1-benzoxazepine derivatives was synthesised to study the influence of the methyl group in the 1-(benzenesulphonyl) moiety, the replacement of the purine by the benzotriazole bioisosteric analogue, and the introduction of a bulky substituent at position 6 of the purine, on the biological effects. Their inhibition against isolated HER2 was studied and the structure-activity relationships have been confirmed by molecular modelling studies. The most potent compound against isolated HER2 is

Indexed as

Drug DesignAntineoplastic AgentsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorErb-b2 Receptor Tyrosine KinasesHumansModels, MolecularMolecular StructureProtein Kinase InhibitorsStructure-Activity RelationshipAntineoplastic AgentsERBB2 protein, humanErb-b2 Receptor Tyrosine KinasesProtein Kinase InhibitorsAntitumourbenzoxazepinesHER2 receptormolecular modellingpyroptosis

Identifiers

PMID34251942
PMCPMC8279156
OpenAlexW3177581362

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.