Evidence map›Paper›PMID 29790770›Full record

ArticleOrganic letters2018

Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors.

Marcel K W Mackwitz, Alexandra Hamacher, Jeremy D Osko, Jana Held, Andrea Schöler, David W Christianson, Matthias U Kassack, Finn K Hansen

Open access · greenAbstract read
In one paragraph

Article in Organic letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.

0numbers the graph read from it
0cells of the map it votes in
32citing papers in PubMed
3.7field-weighted citation impact, top 6% 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

32 citing papers in PubMed, 64 citations in OpenAlex.

  1. Article
  2. Review
  3. Imidazo[1,2‑ACS omega · 2026
    Review
  4. Article
  5. Article
  6. Article
  7. Formaldehyde surrogates in multicomponent reactions.Beilstein journal of organic chemistry · 2025
    Review
  8. Article
  9. Review
  10. Article
  11. Review
  12. Article
  13. Article
  14. Article
  15. Binding of inhibitors to active-site mutants of CD1, the enigmatic catalytic domain of histone deacetylase 6.Acta crystallographica. Section F, Structural biology communications · 2020
    Article
  16. Article
  17. Article
  18. Article
  19. Review
  20. Review
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

8 authors at 4 institutions in 2 countries.

Marcel K W MackwitzInstitut für Pharmazie , Universität Leipzig , Brüderstraße 34 , 04103 Leipzig , Germany.
Alexandra HamacherInstitut für Pharmazeutische und Medizinische Chemie , Heinrich-Heine-Universität Düsseldorf , Universitätsstr. 1 , 40225 Düsseldorf , Germany.
Jeremy D OskoRoy and Diana Vagelos Laboratories, Department of Chemistry , University of Pennsylvania , Philadelphia , Pennsylvania 19104-6323 , United States.
Jana HeldInstitut für Tropenmedizin , Eberhard Karls Universität Tübingen , Wilhelmstr. 27 , 72074 Tübingen , Germany.
Andrea SchölerInstitut für Pharmazie , Universität Leipzig , Brüderstraße 34 , 04103 Leipzig , Germany.
David W ChristiansonRoy and Diana Vagelos Laboratories, Department of Chemistry , University of Pennsylvania , Philadelphia , Pennsylvania 19104-6323 , United States.ORCID 0000-0002-0194-5212
Matthias U KassackInstitut für Pharmazeutische und Medizinische Chemie , Heinrich-Heine-Universität Düsseldorf , Universitätsstr. 1 , 40225 Düsseldorf , Germany.
Finn K HansenInstitut für Pharmazie , Universität Leipzig , Brüderstraße 34 , 04103 Leipzig , Germany.ORCID 0000-0001-9765-5975
Leipzig University · DEHeinrich Heine University Düsseldorf · DEUniversity of Pennsylvania · USUniversity of Tübingen · DE

Funding

X-ray Absorption Spectroscopy (XAS) pp.711-759P41GM103393 · NIGMS · STANFORD UNIVERSITY · PI HODGSON, KEITH O · 2012 to 2019
$30.6M
Structure and Function of MetalloenzymesR01GM049758 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI CHRISTIANSON, DAVID W · 1994 to 2025
$7.6M
NIGMS NIH HHS P41 GM103393NIGMS NIH HHS R01 GM049758
6 · The paper itself

Abstract

The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo[1,2- a]pyridine-based cap groups is presented. The biological evaluation led to the discovery of the hit compound MAIP-032 as a selective HDAC6 inhibitor with promising anticancer activity. The X-ray structure of catalytic domain 2 from Danio rerio HDAC6 complexed with MAIP-032 revealed a monodentate zinc-binding mode.

Indexed as

AnimalsHistone Deacetylase 6Histone Deacetylase InhibitorsImidazolesMolecular StructurePyridinesZebrafishZebrafish ProteinsHDAC6 protein, zebrafishHistone Deacetylase 6Histone Deacetylase InhibitorsImidazolesPyridinesZebrafish Proteins

Identifiers

PMID29790770
PMCPMC5999327
OpenAlexW2804840808

What OpenQuestion holds

Textmetadata
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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.