Evidence map›Paper›PMID 32196342›Full record

ArticleJournal of medicinal chemistry2020

Design, Synthesis, Dynamic Docking, Biochemical Characterization, and

Jose M Arencibia, Nicoletta Brindani, Sebastian Franco-Ulloa, Michela Nigro, Jissy Akkarapattiakal Kuriappan, Giuliana Ottonello, Sine Mandrup Bertozzi, Maria Summa, Stefania Girotto, Rosalia Bertorelli and 2 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.2field-weighted citation impact, top 23% 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

9 citing papers in PubMed, 21 citations in OpenAlex.

  1. Article
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  8. Molecules (Basel, Switzerland) · 2021
    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

12 authors at 1 institution in 1 country.

Jose M ArencibiaMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.ORCID 0000-0003-3227-931X
Nicoletta BrindaniMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Sebastian Franco-UlloaMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.ORCID 0000-0001-6128-0630
Michela NigroMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Jissy Akkarapattiakal KuriappanMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Giuliana OttonelloAnalytical Chemistry and in Vivo Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Sine Mandrup BertozziAnalytical Chemistry and in Vivo Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Maria SummaAnalytical Chemistry and in Vivo Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Stefania GirottoMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Rosalia BertorelliAnalytical Chemistry and in Vivo Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Andrea ArmirottiAnalytical Chemistry and in Vivo Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.ORCID 0000-0002-3766-8755
Marco De VivoMolecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genova, Italy.
Italian Institute of Technology · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

We previously reported a first set of hybrid topoisomerase II (topoII) poisons whose chemical core merges key pharmacophoric elements of etoposide and merbarone, which are two well-known topoII blockers. Here, we report on the expansion of this hybrid molecular scaffold and present 16 more hybrid derivatives that have been designed, synthesized, and characterized for their ability to block topoII and for their overall drug-like profile. Some of these compounds act as topoII poison and exhibit good solubility, metabolic (microsomal) stability, and promising cytotoxicity in three cancer cell lines (DU145, HeLa, A549). Compound

Indexed as

AnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationDNA Topoisomerases, Type IIDrug DesignDrug Screening Assays, AntitumorHumansMiceMolecular Docking SimulationMolecular Dynamics SimulationMolecular StructurePoly-ADP-Ribose Binding ProteinsProtein BindingStructure-Activity RelationshipTopoisomerase II InhibitorsAntineoplastic AgentsDNA Topoisomerases, Type IIPoly-ADP-Ribose Binding ProteinsTOP2A protein, humanTopoisomerase II Inhibitors

Identifiers

PMID32196342
PMCPMC7997578
OpenAlexW3011768394

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.