Evidence map›Paper›PMID 34659728›Full record

ArticleChemical science2021

Borinostats: solid-phase synthesis of carborane-capped histone deacetylase inhibitors with a tailor-made selectivity profile.

Christoph Selg, Andrea Schöler, Julian Schliehe-Diecks, Maria Hanl, Laura Sinatra, Arndt Borkhardt, Menyhárt B Sárosi, Sanil Bhatia, Evamarie Hey-Hawkins, Finn K Hansen

Open access · diamondAbstract read
In one paragraph

Article in Chemical science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.2field-weighted citation impact, top 21% 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

9 citing papers in PubMed, 13 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 3 institutions in 1 country.

Christoph SelgInstitute for Drug Discovery, Medical Faculty, Leipzig University Brüderstraße 34 04103 Leipzig Germany.
Andrea SchölerInstitute for Drug Discovery, Medical Faculty, Leipzig University Brüderstraße 34 04103 Leipzig Germany.
Julian Schliehe-DiecksDepartment of Pediatric Oncology, Hematology and Clinical Immunology, Medical Faculty, Heinrich-Heine University Düsseldorf Düsseldorf Germany.
Maria HanlPharmaceutical Institute, Department of Pharmaceutical and Cell Biological Chemistry, University of Bonn An der Immenburg 4 53121 Bonn Germany finn.hansen@uni-bonn.de.
Laura SinatraInstitute for Drug Discovery, Medical Faculty, Leipzig University Brüderstraße 34 04103 Leipzig Germany.
Arndt BorkhardtDepartment of Pediatric Oncology, Hematology and Clinical Immunology, Medical Faculty, Heinrich-Heine University Düsseldorf Düsseldorf Germany.
Menyhárt B SárosiInstitute of Inorganic Chemistry, Faculty of Chemistry and Mineralogy, Leipzig University Johannisallee 29 04103 Leipzig Germany.ORCID https://orcid.org/0000-0003-4222-0717
Sanil BhatiaDepartment of Pediatric Oncology, Hematology and Clinical Immunology, Medical Faculty, Heinrich-Heine University Düsseldorf Düsseldorf Germany.
Evamarie Hey-HawkinsInstitute of Inorganic Chemistry, Faculty of Chemistry and Mineralogy, Leipzig University Johannisallee 29 04103 Leipzig Germany.ORCID https://orcid.org/0000-0003-4267-0603
Finn K HansenPharmaceutical Institute, Department of Pharmaceutical and Cell Biological Chemistry, University of Bonn An der Immenburg 4 53121 Bonn Germany finn.hansen@uni-bonn.de.ORCID https://orcid.org/0000-0001-9765-5975
Leipzig University · DEHeinrich Heine University Düsseldorf · DEUniversity of Bonn · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The elevated expression of histone deacetylases (HDACs) in various tumor types renders their inhibition an attractive strategy for epigenetic therapeutics. One key issue in the development of improved HDAC inhibitors (HDACis) is the selectivity for single HDAC isoforms over unspecific pan inhibition to minimize off-target toxicity. Utilizing the carborane moiety as a fine-tuning pharmacophore, we herein present a robust solid phase synthetic approach towards tailor-made HDACis meeting both ends of the selectivity spectrum, namely pan inhibition and highly selective HDAC6 inhibition.

Identifiers

PMID34659728
PMCPMC8442681
OpenAlexW3192715508

What Socratic holds

Textmetadata
LicenceCC BY-NC
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 Socratic graph.