Evidence map›Paper›PMID 34008967›Full record

ArticleJournal of medicinal chemistry2021

Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.

De-Xuan Hu, Wen-Lin Tang, Yu Zhang, Hao Yang, Wenjie Wang, Keli Agama, Yves Pommier, Lin-Kun An

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.5field-weighted citation impact, top 18% 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

11 citing papers in PubMed, 26 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 2 institutions in 2 countries.

De-Xuan HuSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Wen-Lin TangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Yu ZhangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Hao YangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Wenjie WangDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda 20892, Maryland, United States.
Keli AgamaDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda 20892, Maryland, United States.
Yves PommierDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda 20892, Maryland, United States.ORCID 0000-0002-3108-0758
Lin-Kun AnSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.ORCID 0000-0002-6088-1503
Sun Yat-sen University · CNNational Institutes of Health · US

Funding

DNA Repair, Cell Cycle Checkpoints and Apoptosis as Targets for Anticancer DrugsZIABC006150 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2009 to 2025
$23.0M
PROTEIN-ASSOCIATED DNA BREAKS AS INDICATOR OF TOPOISOMERASE INHIBITIONZ01BC006150 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 1996 to 2008
$1.5M
Intramural NIH HHS Z01 BC006150
6 · The paper itself

Abstract

As a recently discovered DNA repair enzyme, tyrosyl-DNA phosphodiesterase 1 (TDP1) removes topoisomerase IB (TOP1)-mediated DNA protein cross-links. Inhibiting TDP1 can potentiate the cytotoxicity of TOP1 inhibitors and overcome cancer cell resistance to TOP1 inhibitors. On the basis of our previous study, herein we report the synthesis of benzophenanthridinone derivatives as TOP1 and TDP1 inhibitors. Seven compounds (

Indexed as

Antineoplastic AgentsApoptosisBenzophenanthridinesBinding SitesCell Line, TumorCell SurvivalDNA DamageDNA Topoisomerases, Type IDrug Resistance, NeoplasmDrug Screening Assays, AntitumorHumansMolecular Dynamics SimulationNeoplasmsPhosphodiesterase InhibitorsPhosphoric Diester HydrolasesStructure-Activity RelationshipAntineoplastic AgentsBenzophenanthridinesDNA Topoisomerases, Type IPhosphodiesterase InhibitorsPhosphoric Diester HydrolasesTDP1 protein, humanTOP1 protein, humanTopoisomerase I Inhibitors

Identifiers

PMID34008967
PMCPMC10087287
OpenAlexW3162753652

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.