Evidence map›Paper›PMID 27809521›Full record

ArticleJournal of medicinal chemistry2016

Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue.

Jehad Almaliti, Ayad A Al-Hamashi, Ahmed T Negmeldin, Christin L Hanigan, Lalith Perera, Mary Kay H Pflum, Robert A Casero, L M Viranga Tillekeratne

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
3.0field-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

7 citing papers in PubMed, 29 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

8 authors at 5 institutions in 2 countries.

Jehad AlmalitiDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo , 2801, W. Bancroft Street, Toledo, Ohio 43606, United States.
Ayad A Al-HamashiDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo , 2801, W. Bancroft Street, Toledo, Ohio 43606, United States.
Ahmed T NegmeldinDepartment of Chemistry, Wayne State University , 5101 Cass Avenue, Detroit, Michigan 48202, United States.
Christin L HaniganThe Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine , Bunting/Blaustein Cancer Research Building 1, Room 551, 1650 Orleans Street, Baltimore, Maryland 21231, United States.
Lalith PereraLaboratory of Structural Biology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, North Carolina 27709, United States.
Mary Kay H PflumDepartment of Chemistry, Wayne State University , 5101 Cass Avenue, Detroit, Michigan 48202, United States.
Robert A CaseroThe Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine , Bunting/Blaustein Cancer Research Building 1, Room 551, 1650 Orleans Street, Baltimore, Maryland 21231, United States.
L M Viranga TillekeratneDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo , 2801, W. Bancroft Street, Toledo, Ohio 43606, United States.
Johns Hopkins University · USUniversity of Toledo · USWayne State University · USNational Institutes of Health · USUniversity of Jordan · JO

Funding

Macromolecular ModelingZICES043010 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI COPELAND, WILLIAM · 2012 to 2025
$5.7M
Spermine N1-Acetylase Induction in Lung CancersR01CA051085 · NCI · JOHNS HOPKINS UNIVERSITY · PI CASERO, ROBERT A. · 1990 to 2013
$4.7M
MACROMOLECULAR MODELING AND CARCINOGENESISZ01ES043010 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI DARDEN, THOMAS A · 1986 to 2008
$1.2M
Intramural NIH HHS Z01 ES043010Intramural NIH HHS Z99 ES999999Intramural NIH HHS ZIC ES043010NCI NIH HHS R01 CA051085
6 · The paper itself

Abstract

A number of analogues of the marine-derived histone deacetylase inhibitor largazole incorporating major structural changes in the depsipeptide ring were synthesized. Replacing the thiazole-thiazoline fragment of largazole with a bipyridine group gave analogue 7 with potent cell growth inhibitory activity and an activity profile similar to that of largazole, suggesting that conformational change accompanying switching hybridization from sp

Indexed as

DepsipeptidesDose-Response Relationship, DrugHistone Deacetylase InhibitorsHistone DeacetylasesHumansMolecular Dynamics SimulationMolecular StructureStructure-Activity RelationshipThiazolesDepsipeptidesHistone Deacetylase InhibitorsHistone DeacetylaseslargazoleThiazoles

Identifiers

PMID27809521
PMCPMC5574184
OpenAlexW2546617070

What OpenQuestion holds

Textmetadata
LicenceTDM
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.