Evidence map›Paper›PMID 25083189›Full record

ArticleMedChemComm2014

Selective Inhibition of Bacterial Topoisomerase I by alkynyl-bisbenzimidazoles.

Nihar Ranjan, Geraldine Fulcrand, Ada King, Joseph Brown, Xiuping Jiang, Fenfei Leng, Dev P Arya

Open access · greenAbstract read
In one paragraph

Article in MedChemComm, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

12 citing papers in PubMed, 29 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Perspectives on the Clinical Development of NRF2-Targeting Drugs.Handbook of experimental pharmacology · 2021
    Review
  5. Article
  6. Review
  7. Article
  8. Article
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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

7 authors at 4 institutions in 1 country.

Nihar RanjanDepartment of Chemistry, Clemson University, Clemson, South Carolina, Unite States 29634.
Geraldine FulcrandDepartment of Chemistry and Biochemistry, Florida International University, Miami, Florida 33199 (Unite States).
Ada KingNUBAD, LLC, 900 B West Faris Road, Greenville, South Carolina 29605.
Joseph BrownDepartment of Biological Sciences, Clemson University, Clemson, South Carolina 29634.
Xiuping JiangDepartment of Biological Sciences, Clemson University, Clemson, South Carolina 29634.
Fenfei LengDepartment of Chemistry and Biochemistry, Florida International University, Miami, Florida 33199 (Unite States).
Dev P AryaDepartment of Chemistry, Clemson University, Clemson, South Carolina, Unite States 29634 ; NUBAD, LLC, 900 B West Faris Road, Greenville, South Carolina 29605.
Clemson University · USFlorida International University · USGreenville College · USNubad (United States) · US

Funding

Mechanisms of Transcription-Coupled DNA SupercoilingSC1HD063059 · NICHD · FLORIDA INTERNATIONAL UNIVERSITY · PI LENG, FENFEI · 2009 to 2012
$972k
Development of Ets2-InhibitorsR15CA125724 · NCI · CLEMSON UNIVERSITY · PI ARYA, DEV PRIYA · 2008 to 2009
$398k
Targeting RNA conformation for drug developmentR41GM100607 · NIGMS · NUBAD, LLC · PI ARYA, DEV PRIYA · 2012 to 2012
$295k
NCI NIH HHS R15 CA125724NICHD NIH HHS SC1 HD063059NIGMS NIH HHS R41 GM100607
6 · The paper itself

Abstract

Hoechst dyes are well known DNA binders that non-selectively inhibit the function of mammalian topoisomerase I and II. Herein, we show that Hoechst 33258 based bisbenzimidazoles (DPA 151-154), containing a terminal alkyne, are effective and selective inhibitors of E. coli. topoisomerase I. These bisbenzimidazoles displayed topoisomerase I inhibition much better than Hoechst 33342 or Hoechst 33258 with IC50 values in the range of 2.47-6.63 μM. Bisbenzimidazoles DPA 151-154 also display selective inhibition of E. coli. topoisomerase I over DNA gyrase and Human topoisomerases I and II, and effectively inhibit bacterial growth.

Identifiers

PMID25083189
PMCPMC4112416
OpenAlexW2052118405

What OpenQuestion holds

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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.