Evidence map›Paper›PMID 25890075›Full record

ArticleEuropean journal of medicinal chemistry2015

Discovery of the 2-phenyl-4,5,6,7-Tetrahydro-1H-indole as a novel anti-hepatitis C virus targeting scaffold.

Ivan A Andreev, Dinesh Manvar, Maria Letizia Barreca, Dmitry S Belov, Amartya Basu, Noreena L Sweeney, Nina K Ratmanova, Evgeny R Lukyanenko, Giuseppe Manfroni, Violetta Cecchetti and 4 more

Open access · greenAbstract 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 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.8field-weighted citation impact, top 15% 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, 31 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Crystal structure of 3-(2-nitro-phen-yl)-1-(1-phenyl-sulfonyl-1H-indol-3-yl)propan-1-one.Acta crystallographica. Section E, Crystallographic communications · 2015
    Article
  6. Crystal structure of N-{[3-bromo-1-(phenyl-sulfon-yl)-1H-indol-2-yl]meth-yl}benzene-sulfonamide.Acta crystallographica. Section E, Crystallographic communications · 2015
    Article
  7. Crystal structure of methyl (2Z)-3-(4-chloro-phen-yl)-2-[(3-methyl-1H-indol-1-yl)meth-yl]prop-2-enoate.Acta crystallographica. Section E, Crystallographic communications · 2015
    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

14 authors at 5 institutions in 3 countries.

Ivan A AndreevEDASA Scientific Srls., Via Stingi, 37, 66050 San Salvo, CH, Italy; Chemistry Department of Lomonosov Moscow State University, Moscow, 119991, GSP-2, Leninskie Gory, 1/3, Russia.
Dinesh ManvarDepartment of Microbiology, Biochemistry and Molecular Genetics, Rutgers, The State University of New Jersey, New Jersey Medical School, NJ 07103, USA.
Maria Letizia BarrecaDepartment of Pharmaceutical Sciences, University of Perugia, Via A. Fabretti, 48, 06123 Perugia, Italy. Electronic address: lbarreca@unipg.it.
Dmitry S BelovEDASA Scientific Srls., Via Stingi, 37, 66050 San Salvo, CH, Italy; Chemistry Department of Lomonosov Moscow State University, Moscow, 119991, GSP-2, Leninskie Gory, 1/3, Russia.
Amartya BasuDepartment of Microbiology, Biochemistry and Molecular Genetics, Rutgers, The State University of New Jersey, New Jersey Medical School, NJ 07103, USA.
Noreena L SweeneyDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, 3210 N. Cramer St., Milwaukee, WI 53211, USA.
Nina K RatmanovaChemistry Department of Lomonosov Moscow State University, Moscow, 119991, GSP-2, Leninskie Gory, 1/3, Russia.
Evgeny R LukyanenkoEDASA Scientific Srls., Via Stingi, 37, 66050 San Salvo, CH, Italy.
Giuseppe ManfroniDepartment of Pharmaceutical Sciences, University of Perugia, Via A. Fabretti, 48, 06123 Perugia, Italy.
Violetta CecchettiDepartment of Pharmaceutical Sciences, University of Perugia, Via A. Fabretti, 48, 06123 Perugia, Italy.
David N FrickDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, 3210 N. Cramer St., Milwaukee, WI 53211, USA.
Andrea AltieriEDASA Scientific Srls., Via Stingi, 37, 66050 San Salvo, CH, Italy. Electronic address: aaltieri@edasascientific.com.
Neerja Kaushik-BasuDepartment of Microbiology, Biochemistry and Molecular Genetics, Rutgers, The State University of New Jersey, New Jersey Medical School, NJ 07103, USA. Electronic address: kaushik@njms.rutgers.edu.
Alexander V KurkinChemistry Department of Lomonosov Moscow State University, Moscow, 119991, GSP-2, Leninskie Gory, 1/3, Russia.
Lomonosov Moscow State University · RURutgers, The State University of New Jersey · USUniversity of Perugia · ITUniversity of Wisconsin–Milwaukee · USTakasago (United States) · US

Funding

Heparan sulfate proteoglycans in signaling and developmentR35GM131688 · NIGMS · UNIVERSITY OF MINNESOTA · PI Hiroshi Nakato · 2019 to 2026
$2.6M
Antiviral potential of helicase inhibitorsR01AI088001 · NIAID · UNIVERSITY OF WISCONSIN MILWAUKEE · PI FRICK, DAVID N · 2010 to 2012
$1.1M
NIAID NIH HHS R01 AI088001NIGMS NIH HHS R35 GM131688
6 · The paper itself

Abstract

Although all-oral direct-acting antiviral (DAA) therapy for hepatitis C virus (HCV) treatment is now a reality, today's HCV drugs are expensive, and more affordable drugs are still urgently needed. In this work, we report the identification of the 2-phenyl-4,5,6,7-Tetrahydro-1H-indole chemical scaffold that inhibits cellular replication of HCV genotype 1b and 2a subgenomic replicons. The anti-HCV genotype 1b and 2a profiling and effects on cell viability of a selected representative set of derivatives as well as their chemical synthesis are described herein. The most potent compound 39 displayed EC50 values of 7.9 and 2.6 μM in genotype 1b and 2a, respectively. Biochemical assays showed that derivative 39 had no effect on HCV NS5B polymerase, NS3 helicase, IRES mediated translation and selected host factors. Thus, future work will involve both the chemical optimization and target identification of 2-phenyl-4,5,6,7-Tetrahydro-1H-indoles as new anti-HCV agents.

Indexed as

Drug DiscoveryAntiviral AgentsCell LineDose-Response Relationship, DrugHepacivirusHumansIndolesMicrobial Sensitivity TestsStructure-Activity Relationship2-phenyl-4,5,6,7-tetrahydro-1H-indoleAntiviral AgentsIndoles4,5,6,7-Tetrahydro-1H-indoleAnti-HCV agentsHepatitis C virus

Identifiers

PMID25890075
PMCPMC5557381
OpenAlexW2022972598

What OpenQuestion holds

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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.