Evidence map›Paper›PMID 31690062›Full record

ArticleMolecules (Basel, Switzerland)2019

Synthesis and Antiviral Activity of Novel 1,3,4-Thiadiazole Inhibitors of DDX3X.

Annalaura Brai, Stefania Ronzini, Valentina Riva, Lorenzo Botta, Claudio Zamperini, Matteo Borgini, Claudia Immacolata Trivisani, Anna Garbelli, Carla Pennisi, Adele Boccuto and 4 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed, 1 pooled it
3.5field-weighted citation impact, top 7% 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

16 citing papers in PubMed, 1 synthesis or guideline pooled it, 41 citations in OpenAlex.

  1. Recent Advances in Nitrogen-Containing Heterocyclic Scaffolds as Antiviral Agents.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2024
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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

14 authors at 2 institutions in 2 countries.

Annalaura BraiDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. annalaura.brai@gmail.com.ORCID 0000-0001-6395-9348
Stefania RonziniDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. ronzinis@gmail.com.ORCID 0000-0002-5003-2639
Valentina RivaIstituto di Genetica Molecolare, IGM-CNR "Luigi Luca Cavalli-Sforza", Via Abbiategrasso 207, I-27100 Pavia, Italy. valentina.riva01@universitadipavia.it.
Lorenzo BottaDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. lor.botta83@gmail.com.
Claudio ZamperiniDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. claudiozamperini@yahoo.it.ORCID 0000-0001-9321-2886
Matteo BorginiDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. borgini.m4@gmail.com.ORCID 0000-0001-6285-7374
Claudia Immacolata TrivisaniDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. c.trivisani@gmail.com.
Anna GarbelliIstituto di Genetica Molecolare, IGM-CNR "Luigi Luca Cavalli-Sforza", Via Abbiategrasso 207, I-27100 Pavia, Italy. agarbelli@gmail.com.
Carla PennisiIstituto di Genetica Molecolare, IGM-CNR "Luigi Luca Cavalli-Sforza", Via Abbiategrasso 207, I-27100 Pavia, Italy. carlapennisi@outlook.it.
Adele BoccutoDipartimento di Biotecnologie Mediche, Università degli Studi di Siena, 53100 Siena, Italy. adele.boccuto@gmail.com.
Francesco SaladiniDipartimento di Biotecnologie Mediche, Università degli Studi di Siena, 53100 Siena, Italy. france.saladini@gmail.com.
Maurizio ZazziDipartimento di Biotecnologie Mediche, Università degli Studi di Siena, 53100 Siena, Italy. maurizio.zazzi@gmail.com.ORCID 0000-0002-0344-6281
Giovanni MagaIstituto di Genetica Molecolare, IGM-CNR "Luigi Luca Cavalli-Sforza", Via Abbiategrasso 207, I-27100 Pavia, Italy. giovanni.maga@igm.cnr.it.
Maurizio BottaDipartimento Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, I-53100 Siena, Italy. botta.maurizio@gmail.com.
University of Siena · ITIstituto di Genetica Molecolare · IT

Funding

Consiglio Nazionale delle Ricerche Identification of novel molecules with therapeutic potential against Zika virus and other emerging virusesFirst Health Pharmaceuticals DDX3X inhibitors
6 · The paper itself

Abstract

The human ATPase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against both infectious diseases and cancer. Herein, a new family of DDX3X inhibitors was designed, synthesized, and tested for its inhibitory action on the ATPase activity of the enzyme. The potential use of the most promising derivatives it has been investigated by evaluating their anti-HIV-1 effects, revealing inhibitory activities in the low micromolar range. A preliminary ADME analysis demonstrated high metabolic stability and good aqueous solubility. The promising biological profile, together with the suitable in vitro pharmacokinetic properties, make these novel compounds a very good starting point for further development.

Indexed as

Antiviral AgentsDEAD-box RNA HelicasesHIV-1HumansThiadiazolesVirus Replication1,3,4-thiadiazoleAntiviral AgentsDDX3X protein, humanDEAD-box RNA HelicasesThiadiazolesantiviralsDDX3XHIV-1host proteins

Identifiers

PMID31690062
PMCPMC6864647
OpenAlexW2985164319

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.