Evidence map›Paper›PMID 35073610›Full record

ArticleChemMedChem2022

Balancing Histone Deacetylase (HDAC) Inhibition and Drug-likeness: Biological and Physicochemical Evaluation of Class I Selective HDAC Inhibitors.

Linda Schäker-Hübner, Reza Haschemi, Thomas Büch, Fabian B Kraft, Birke Brumme, Andrea Schöler, Robert Jenke, Jens Meiler, Achim Aigner, Gerd Bendas and 1 more

Open access · hybridAbstract read
In one paragraph

Article in ChemMedChem, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
2.8field-weighted citation impact, top 9% 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

22 citing papers in PubMed, 36 citations in OpenAlex.

  1. Article
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  15. Article
  16. Discovery of novel polysubstitutedJournal of enzyme inhibition and medicinal chemistry · 2023
    Article
  17. Article
  18. Article
  19. Review
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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

11 authors at 3 institutions in 1 country.

Linda Schäker-HübnerInstitut für Wirkstoffentwicklung, Medizinische Fakultät, Universität Leipzig, Brüderstraße 34, 04103, Leipzig, Germany.
Reza HaschemiAbteilung für Pharmazeutische und Zellbiologische Chemie, Pharmazeutisches Institut, Universität Bonn, An der Immenburg 4, 53121, Bonn, Germany.
Thomas BüchRudolf-Boehm-Institut für Pharmakologie und Toxikologie, Klinische Pharmakologie, Medizinische Fakultät, Universität Leipzig, Härtelstraße 16-18, 04107, Leipzig, Germany.ORCID 0000-0002-8609-9034
Fabian B KraftAbteilung für Pharmazeutische und Zellbiologische Chemie, Pharmazeutisches Institut, Universität Bonn, An der Immenburg 4, 53121, Bonn, Germany.
Birke BrummeInstitut für Wirkstoffentwicklung, Medizinische Fakultät, Universität Leipzig, Brüderstraße 34, 04103, Leipzig, Germany.
Andrea SchölerInstitut für Wirkstoffentwicklung, Medizinische Fakultät, Universität Leipzig, Brüderstraße 34, 04103, Leipzig, Germany.
Robert JenkeRudolf-Boehm-Institut für Pharmakologie und Toxikologie, Klinische Pharmakologie, Medizinische Fakultät, Universität Leipzig, Härtelstraße 16-18, 04107, Leipzig, Germany.ORCID 0000-0002-4027-1249
Jens MeilerInstitut für Wirkstoffentwicklung, Medizinische Fakultät, Universität Leipzig, Brüderstraße 34, 04103, Leipzig, Germany.
Achim AignerRudolf-Boehm-Institut für Pharmakologie und Toxikologie, Klinische Pharmakologie, Medizinische Fakultät, Universität Leipzig, Härtelstraße 16-18, 04107, Leipzig, Germany.ORCID 0000-0002-2778-6256
Gerd BendasAbteilung für Pharmazeutische und Zellbiologische Chemie, Pharmazeutisches Institut, Universität Bonn, An der Immenburg 4, 53121, Bonn, Germany.
Finn K HansenAbteilung für Pharmazeutische und Zellbiologische Chemie, Pharmazeutisches Institut, Universität Bonn, An der Immenburg 4, 53121, Bonn, Germany.ORCID 0000-0001-9765-5975
Leipzig University · DEUniversity of Bonn · DEUniversity Hospital Leipzig · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Herein we report the structure-activity and structure-physicochemical property relationships of a series of class I selective ortho-aminoanilides targeting the "foot-pocket" in HDAC1&2. To balance the structural benefits and the physicochemical disadvantages of these substances, we started with a set of HDACi related to tacedinaline (CI-994) and evaluated their solubility, lipophilicity (log D

Indexed as

Histone Deacetylase InhibitorsPeptoidsHistone Deacetylase 1Histone DeacetylasesHistone Deacetylase 1Histone Deacetylase InhibitorsHistone DeacetylasesPeptoidscancerdrug designepigeneticshistone deacetylasesinhibitors

Identifiers

PMID35073610
PMCPMC9303312
OpenAlexW4206962742

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.