Evidence map›Paper›PMID 34509798›Full record

ArticleBioorganic chemistry2021

A new class of cytotoxic agents targets tubulin and disrupts microtubule dynamics.

Ayad A Al-Hamashi, Radhika Koranne, Samkeliso Dlamini, Abdulateef Alqahtani, Endri Karaj, Maisha S Rashid, Joseph R Knoff, Matthew Dunworth, Mary Kay H Pflum, Robert A Casero and 3 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic chemistry, 2021. 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
0.9field-weighted citation impact, top 27% 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, 18 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

13 authors at 5 institutions in 1 country.

Ayad A Al-HamashiDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Radhika KoranneDepartment of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Samkeliso DlaminiDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Abdulateef AlqahtaniDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Endri KarajDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Maisha S RashidDepartment of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Joseph R KnoffDepartment of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202, USA.
Matthew DunworthThe Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine, Bunting/Blaustein Cancer Research Building 1 1650 Orleans Street - Room 551, Baltimore, MD 21231, USA.
Mary Kay H PflumDepartment of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202, USA.
Robert A CaseroThe Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine, Bunting/Blaustein Cancer Research Building 1 1650 Orleans Street - Room 551, Baltimore, MD 21231, USA.
Lalith PereraLaboratory of Genome Integrity and Structural Biology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, NC 27709, USA.
William R TaylorDepartment of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA. Electronic address: william.tayor2@utoledo.edu.
L M Viranga TillekeratneDepartment of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA. Electronic address: ltillek@utnet.utoledo.edu.
University of Toledo · USWayne State University · USJohns Hopkins University · USNational Institute of Environmental Health Sciences · USSidney Kimmel Comprehensive Cancer Center · US

Funding

Chemical Approaches to Study Protein Post-Translational ModificationsR35GM131821 · NIGMS · WAYNE STATE UNIVERSITY · PI Mary Kay H Pflum · 2019 to 2026
$4.3M
MACROMOLECULAR MODELING AND CARCINOGENESISZ01ES043010 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI DARDEN, THOMAS A · 1986 to 2008
$1.2M
Identification of Histone Deacetylase Substrates using Trapping MutantsR01GM121061 · NIGMS · WAYNE STATE UNIVERSITY · PI PFLUM, MARY KAY H · 2016 to 2018
$829k
Novel Small Molecule Ferroptotic Compounds to Target Mesenchymal Breast Cancer and Breast Cancer Stem CellsR15CA213185 · NCI · UNIVERSITY OF TOLEDO · PI TILLEKERATNE, VIRANGA · 2018 to 2018
$449k
Regulation of the Mitotic Checkpoint by Gsk3R15GM120712 · NIGMS · UNIVERSITY OF TOLEDO · PI TAYLOR, WILLIAM R. · 2017 to 2017
$443k
Intramural NIH HHS Z01 ES043010NCI NIH HHS R15 CA213185NIGMS NIH HHS R01 GM121061NIGMS NIH HHS R15 GM120712NIGMS NIH HHS R35 GM131821
6 · The paper itself

Abstract

Despite the advances in treatment strategies, cancer is still the second leading cause of death in the USA. A majority of the currently used cancer drugs have limitations in their clinical use due to poor selectivity, toxic side effects and multiple drug resistance, warranting the development of new anticancer drugs of different mechanisms of action. Here we describe the design, synthesis and initial biological evaluation of a new class of antimitotic agents that modulate tubulin polymerization. Structurally, these compounds are chalcone mimics containing a 1-(1H-imidazol-2-yl)ethan-1-one moiety, which was initially introduced to act as a metal-binding group and inhibit histone deacetylase enzymes. Although several analogues selectively inhibited purified HDAC8 with IC

Indexed as

Antineoplastic AgentsCell ProliferationCell SurvivalCytotoxinsDose-Response Relationship, DrugDrug Screening Assays, AntitumorEthanolHCT116 CellsHumansImidazolesMicrotubulesMolecular StructurePolymerizationStructure-Activity RelationshipTubulinTubulin ModulatorsAntineoplastic AgentsCytotoxinsEthanolImidazolesTubulinTubulin ModulatorsAnticancer agentsAntimitotic agentsChalconesMitotic arrestMitotic spindle

Identifiers

PMID34509798
PMCPMC8530978
OpenAlexW3196703635

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.