Evidence map›Paper›PMID 26188908›Full record

ArticleEuropean journal of medicinal chemistry2015

Synthesis and biological evaluation of 6-substituted indolizinoquinolinediones as catalytic DNA topoisomerase I inhibitors.

Le-Mao Yu, Xiao-Ru Zhang, Xiao-Bing Li, Yuan Yang, Hong-Yu Wei, Xi-Xin He, Lian-Quan Gu, Zhi-Shu Huang, Yves Pommier, Lin-Kun An

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
–field-weighted citation impact
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

5 citing papers in PubMed.

  1. Article
  2. The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor.Journal of enzyme inhibition and medicinal chemistry · 2019
    Article
  3. Article
  4. Article
  5. Article
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

10 authors.

Le-Mao YuSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Xiao-Ru ZhangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Xiao-Bing LiSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Yuan YangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Hong-Yu WeiCollege of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Xi-Xin HeCollege of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Lian-Quan GuSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Zhi-Shu HuangSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Yves PommierDevelopmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-4255, United States.
Lin-Kun AnSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: lssalk@mail.sysu.edu.cn.

Funding

DNA Topoisomerases as Target of Action of Anticancer DrugsZIABC006161 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2009 to 2025
$16.8M
DNA TOPOISOMERASES AS TARGET OF ACTION OF ANTICANCER DRUGSZ01BC006161 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 1996 to 2008
$1.5M
Intramural NIH HHS Z01 BC006161
6 · The paper itself

Abstract

In our previous work, indolizinoquinolinedione derivative 1 was identified as a Top1 catalytic inhibitor. Herein, a series of 6-substituted indolizinoquinolinedione derivatives were synthesized through modification of the parent compound 1. Top1 cleavage and relaxation assays indicate that none of these novel compounds act as classical Top1 poison, and that the compounds with alkylamino terminus at C-6 side chain, including 8, 11-16, 18-21, 25, 26 and 28-30, are the most potent Top1 catalytic inhibitors. Top1-mediated unwinding assay demonstrated that 14, 22 and 26 were Top1 catalytic inhibitors without Top1-mediated unwinding effect. Moreover, MTT results showed that compounds 26, 28-30 exhibit significant cytotoxicity against human leukemia HL-60 cells, and that compound 26 exerts potent cytotoxicity against A549 lung cancer cells at nanomolar range.

Indexed as

Antineoplastic AgentsBiocatalysisCell ProliferationDNA Topoisomerases, Type IDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansIndolizinesMolecular StructureQuinolonesStructure-Activity RelationshipTopoisomerase I InhibitorsTumor Cells, CulturedAntineoplastic AgentsDNA Topoisomerases, Type IIndolizinesN-(3-(4-methylpiperazin-1-yl)propyl)-5,12-dioxo-5,12-dihydroindolizino(2,3-g)quinoline-6-carboxamideQuinolonesTopoisomerase I InhibitorsAnticancerDNA topoisomeraseIndolizinoquinolinedioneInhibitor

Identifiers

PMID26188908
PMCPMC4558194

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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.