Evidence map›Paper›PMID 32348628›Full record

ArticleChemMedChem2020

Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors.

Michael Morgen, Raphael R Steimbach, Magalie Géraldy, Lars Hellweg, Peter Sehr, Johannes Ridinger, Olaf Witt, Ina Oehme, Corey J Herbst-Gervasoni, Jeremy D Osko and 4 more

Open access · hybridAbstract read
In one paragraph

Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
2.1field-weighted citation impact, top 12% 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

16 citing papers in PubMed, 37 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

14 authors at 3 institutions in 2 countries.

Michael MorgenCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.ORCID 0000-0001-9539-6404
Raphael R SteimbachCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.
Magalie GéraldyCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.
Lars HellwegCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.
Peter SehrChemical Biology Core Facility, European Molecular Biology Laboratory (EMBL), 69117, Heidelberg, Germany.
Johannes RidingerHopp Children's Cancer Center Heidelberg (KiTZ), 69120, Heidelberg, Germany.ORCID 0000-0003-1341-7721
Olaf WittHopp Children's Cancer Center Heidelberg (KiTZ), 69120, Heidelberg, Germany.
Ina OehmeHopp Children's Cancer Center Heidelberg (KiTZ), 69120, Heidelberg, Germany.ORCID 0000-0002-0827-2356
Corey J Herbst-GervasoniRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.ORCID 0000-0002-7154-4123
Jeremy D OskoRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.ORCID 0000-0001-8595-4759
Nicholas J PorterRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.
David W ChristiansonRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104-6323, USA.
Nikolas GunkelCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.
Aubry K MillerCancer Drug Development Group, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120, Heidelberg, Germany.ORCID 0000-0002-1761-4143
German Cancer Research Center · DEUniversity of Pennsylvania · USEuropean Molecular Biology Laboratory · DE

Funding

User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI Nozomi Ando, J Christopher Fromme · 2018 to 2026
$34.2M
Structure and Function of MetalloenzymesR01GM049758 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI CHRISTIANSON, DAVID W · 1994 to 2025
$7.6M
Predoctoral Training at the Chemistry-Biology InterfaceT32GM071339 · NIGMS · WISTAR INSTITUTE · PI MARMORSTEIN, RONEN, SPEICHER, DAVID W. · 2005 to 2019
$3.2M
Pixel Array Detector for X-ray CrystallographyS10RR029205 · NCRR · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2010 to 2010
$1.8M
NCRR NIH HHS S10 RR029205NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R01 GM049758NIGMS NIH HHS T32 GM071339
6 · The paper itself

Abstract

We report the synthesis and evaluation of a class of selective multitarget agents for the inhibition of HDAC6, HDAC8, and HDAC10. The concept for this study grew out of a structural analysis of the two selective inhibitors Tubastatin A (HDAC6/10) and PCI-34051 (HDAC8), which we recognized share the same N-benzylindole core. Hybridization of the two inhibitor structures resulted in dihydroxamic acids with benzyl-indole and -indazole core motifs. These substances exhibit potent activity against HDAC6, HDAC8, and HDAC10, while retaining selectivity over HDAC1, HDAC2, and HDAC3. The best substance inhibited the viability of the SK-N-BE(2)C neuroblastoma cell line with an IC

Indexed as

Drug DesignCell ProliferationCell SurvivalDose-Response Relationship, DrugHistone Deacetylase 6Histone Deacetylase InhibitorsHistone DeacetylasesHumansHydroxamic AcidsMolecular StructureRepressor ProteinsStructure-Activity RelationshipTumor Cells, CulturedHDAC6 protein, humanHDAC8 protein, humanHistone Deacetylase 6Histone Deacetylase InhibitorsHistone DeacetylasesHydroxamic AcidsRepressor ProteinsHDAC10HDAC8inhibitorspolypharmacologytargeted therapy

Identifiers

PMID32348628
PMCPMC7335359
OpenAlexW3018429597

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.