Evidence map›Paper›PMID 34832901›Full record

ArticlePharmaceuticals (Basel, Switzerland)2021

Synthesis and Antiproliferative Evaluation of 3-Chloroazetidin-2-ones with Antimitotic Activity: Heterocyclic Bridged Analogues of Combretastatin A-4.

Azizah M Malebari, Shu Wang, Thomas F Greene, Niamh M O'Boyle, Darren Fayne, Mohemmed Faraz Khan, Seema M Nathwani, Brendan Twamley, Thomas McCabe, Daniela M Zisterer and 1 more

Erratum issuedOpen access · goldAbstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
1.2field-weighted citation impact, top 23% 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

8 citing papers in PubMed, 18 citations in OpenAlex.

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  7. Virus-Induced Membrane Fusion in Neurodegenerative Disorders.Frontiers in cellular and infection microbiology · 2022
    Review
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4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

11 authors at 2 institutions in 2 countries.

Azizah M MalebariDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Shu WangSchool of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Thomas F GreeneSchool of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Niamh M O'BoyleSchool of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.ORCID 0000-0001-5660-4944
Darren FayneMolecular Design Group, School of Biochemistry and Immunology, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Mohemmed Faraz KhanMolecular Design Group, School of Biochemistry and Immunology, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.ORCID 0000-0003-3846-1577
Seema M NathwaniSchool of Biochemistry and Immunology, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Brendan TwamleySchool of Chemistry, Trinity College Dublin, 2 DO2R590 Dublin, Ireland.
Thomas McCabeSchool of Chemistry, Trinity College Dublin, 2 DO2R590 Dublin, Ireland.
Daniela M ZistererSchool of Biochemistry and Immunology, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Mary J MeeganSchool of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.
Trinity College Dublin · IEKing Abdulaziz University · SA

Funding

King Abdulaziz University IRKA1001Trinity College Dublin Post graduate Scholarship
6 · The paper itself

Abstract

Antimitotic drugs that target tubulin are among the most widely used chemotherapeutic agents; however, the development of multidrug resistance has limited their clinical activity. We report the synthesis and biological properties of a series of novel 3-chloro-β-lactams and 3,3-dichloro-β-lactams (2-azetidinones) that are structurally related to the tubulin polymerisation inhibitor and vascular targeting agent, Combretastatin A-4. These compounds were evaluated as potential tubulin polymerisation inhibitors and for their antiproliferative effects in breast cancer cells. A number of the compounds showed potent activity in MCF-7 breast cancer cells, e.g., compound

Indexed as

3-chloroazetidin-2-onesantimitoticantiproliferative activitybreast cancercolchicine-binding sitecombretastatin A-4tubulin polymerisationβ-lactam

Identifiers

PMID34832901
PMCPMC8624998
OpenAlexW3208725076

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.