Evidence map›Paper›PMID 34106711›Full record

ArticleJournal of medicinal chemistry2021

Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.

Antonella Messore, Angela Corona, Valentina Noemi Madia, Francesco Saccoliti, Valeria Tudino, Alessandro De Leo, Davide Ialongo, Luigi Scipione, Daniela De Vita, Giorgio Amendola and 9 more

Open access · hybridAbstract 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 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 30% 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

5 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
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  5. 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

19 authors at 7 institutions in 2 countries.

Antonella MessoreDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.
Angela CoronaDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.ORCID 0000-0002-6630-8636
Valentina Noemi MadiaDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.
Francesco SaccolitiD3 PharmaChemistry, Italian Institute of Technology, Via Morego 30, I-16163 Genova, Italy.
Valeria TudinoDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.
Alessandro De LeoDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.
Davide IalongoDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.
Luigi ScipioneDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.ORCID 0000-0002-2006-7005
Daniela De VitaDepartment of Environmental Biology, "Sapienza" University of Rome, p.le Aldo Moro 5, I-00185 Rome, Italy.
Giorgio AmendolaDiSTABiF, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.ORCID 0000-0003-4271-5031
Ettore NovellinoDepartment of Pharmacy, University Federico II of Naples, Via D. Montesano 49, 80131 Naples, Italy.ORCID 0000-0002-2181-2142
Sandro CosconatiDiSTABiF, University of Campania "Luigi Vanvitelli", Via Vivaldi 43, 81100 Caserta, Italy.ORCID 0000-0002-8900-0968
Mathieu MétifiotLaboratoire MFP, UMR 5234, CNRS - Université de Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux cedex, France.
Marie-Line AndreolaLaboratoire MFP, UMR 5234, CNRS - Université de Bordeaux, 146 rue Léo Saignat, 33076 Bordeaux cedex, France.
Francesca EspositoDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.
Nicole GrandiDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.
Enzo TramontanoDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554-09042 Monserrato (CA), Italy.ORCID 0000-0002-4849-0980
Roberta CostiDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.ORCID 0000-0002-1314-9029
Roberto Di SantoDipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185 Rome, Italy.ORCID 0000-0002-4279-7666
Istituto Pasteur · ITUniversity of Cagliari · ITCentre National de la Recherche Scientifique · FRUniversity of Campania "Luigi Vanvitelli" · ITItalian Institute of Technology · ITSapienza University of Rome · ITUniversity of Naples Federico II · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Novel anti-HIV agents are still needed to overcome resistance issues, in particular inhibitors acting against novel viral targets. The ribonuclease H (RNase H) function of the reverse transcriptase (RT) represents a validated and promising target, and no inhibitor has reached the clinical pipeline yet. Here, we present rationally designed non-diketo acid selective RNase H inhibitors (RHIs) based on the quinolinone scaffold starting from former dual integrase (IN)/RNase H quinolinonyl diketo acids. Several derivatives were synthesized and tested against RNase H and viral replication and found active at micromolar concentrations. Docking studies within the RNase H catalytic site, coupled with site-directed mutagenesis, and Mg

Indexed as

Anti-HIV AgentsHeLa CellsHIV-1HumansMagnesiumMicrobial Sensitivity TestsMolecular Docking SimulationMutagenesis, Site-DirectedMutationProtein BindingQuinolonesReverse Transcriptase InhibitorsRibonuclease H, Human Immunodeficiency VirusVirus ReplicationAnti-HIV AgentsMagnesiumQuinolonesReverse Transcriptase InhibitorsRibonuclease H, Human Immunodeficiency Virus

Identifiers

PMID34106711
PMCPMC8279492
OpenAlexW3168002634

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.