Evidence map›Paper›PMID 28829913›Full record

ArticleJournal of medicinal chemistry2017

Virtual Screening of Acyclovir Derivatives as Potential Antiviral Agents: Design, Synthesis, and Biological Evaluation of New Acyclic Nucleoside ProTides.

Marco Derudas, Christophe Vanpouille, Davide Carta, Sonia Zicari, Graciela Andrei, Robert Snoeck, Andrea Brancale, Leonid Margolis, Jan Balzarini, Christopher McGuigan

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.8field-weighted citation impact, top 29% 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

4 citing papers in PubMed, 15 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
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 at 3 institutions in 3 countries.

Marco DerudasCardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University , Cardiff, CF10 3NB, U.K.ORCID 0000-0003-1731-2855
Christophe VanpouilleEunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health , Bethesda, Maryland 20892, United States.
Davide CartaCardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University , Cardiff, CF10 3NB, U.K.
Sonia ZicariEunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health , Bethesda, Maryland 20892, United States.
Graciela AndreiRega Institute for Medical Research, KU Leuven , B-3000 Leuven, Belgium.
Robert SnoeckRega Institute for Medical Research, KU Leuven , B-3000 Leuven, Belgium.
Andrea BrancaleCardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University , Cardiff, CF10 3NB, U.K.
Leonid MargolisEunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health , Bethesda, Maryland 20892, United States.
Jan BalzariniRega Institute for Medical Research, KU Leuven , B-3000 Leuven, Belgium.
Christopher McGuiganCardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University , Cardiff, CF10 3NB, U.K.
National Institutes of Health · USCardiff University · GBRega Institute for Medical Research · BE

Funding

Cell Interactions in Three Dimensional Tissue CultureZIAHD001416 · NICHD · EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH & HUMAN DEVELOPMENT · PI MARGOLIS, LEONID B. · 2009 to 2017
$15.7M
Viral transmission and pathogenesis in human tissuesZIAHD008968 · NICHD · EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH & HUMAN DEVELOPMENT · PI MARGOLIS, LEONID B. · 2018 to 2023
$12.2M
TISSUE IMAGING IN CELL BIOLOGYZ01HD001416 · NICHD · EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH & HUMAN DEVELOPMENT · PI MARGOLIS, LEONID B. · 1993 to 2008
$2.7M
Intramural NIH HHS Z01 HD001416
6 · The paper itself

Abstract

Following our findings on the anti-human immunodeficiency virus (HIV) activity of acyclovir (ACV) phosphate prodrugs, we herein report the ProTide approach applied to a series of acyclic nucleosides aimed at the identification of novel and selective antiviral, in particular anti-HIV agents. Acyclic nucleoside analogues used in this study were identified through a virtual screening using HIV-reverse transcriptase (RT), adenylate/guanylate kinase, and human DNA polymerase γ. A total of 39 new phosphate prodrugs were synthesized and evaluated against HIV-1 (in vitro and ex vivo human tonsillar tissue system) and human herpes viruses. Several ProTide compounds showed substantial potency against HIV-1 at low micromolar range while the parent nucleosides were not effective. Also, pronounced inhibition of herpesvirus replication was observed. A carboxypeptidase-mediated hydrolysis study was performed for a selection of compounds to assess the formation of putative metabolites and support the biological activity observed.

Indexed as

AcyclovirAnti-HIV AgentsCell LineDrug DesignHerpes SimplexHIV-1HIV InfectionsHIV Reverse TranscriptaseHumansMolecular Docking SimulationNucleosidesSimplexvirusVirus ReplicationAcyclovirAnti-HIV AgentsHIV Reverse TranscriptaseNucleosides

Identifiers

PMID28829913
PMCPMC5731253
OpenAlexW2746166896

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.