Evidence map›Paper›PMID 24651068›Full record

ArticlePloS one2014

Theoretical and experimental studies of new modified isoflavonoids as potential inhibitors of topoisomerase I from Plasmodium falciparum.

Wilian A Cortopassi, Julia Penna-Coutinho, Anna C C Aguiar, André S Pimentel, Camilla D Buarque, Paulo R R Costa, Bruna R M Alves, Tanos C C França, Antoniana U Krettli

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 33% 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

6 citing papers in PubMed, 19 citations in OpenAlex.

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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

9 authors at 4 institutions in 1 country.

Wilian A CortopassiDepartamento de Química, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, Brazil; Laboratório de Modelagem Aplicada a Defesa Química e Biológica, Instituto Militar de Engenharia, Rio de Janeiro, Brazil.
Julia Penna-CoutinhoLaboratório de Malária, Centro de Pesquisas René Rachou, Fundação Instituto Oswaldo Cruz, Belo Horizonte, Brazil; Faculdade de Medicina, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
Anna C C AguiarLaboratório de Malária, Centro de Pesquisas René Rachou, Fundação Instituto Oswaldo Cruz, Belo Horizonte, Brazil; Faculdade de Medicina, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
André S PimentelDepartamento de Química, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, Brazil.
Camilla D BuarqueDepartamento de Química, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, Brazil.
Paulo R R CostaLaboratório de Química Bioorgânica, Núcleo de Pesquisas de Produtos Naturais, Rio de Janeiro, Brazil.
Bruna R M AlvesDepartamento de Química, Pontifícia Universidade Católica do Rio de Janeiro, Rio de Janeiro, Brazil.
Tanos C C FrançaLaboratório de Modelagem Aplicada a Defesa Química e Biológica, Instituto Militar de Engenharia, Rio de Janeiro, Brazil.
Antoniana U KrettliLaboratório de Malária, Centro de Pesquisas René Rachou, Fundação Instituto Oswaldo Cruz, Belo Horizonte, Brazil; Faculdade de Medicina, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
Pontifical Catholic University of Rio de Janeiro · BRFundação Oswaldo Cruz · BRMilitary Institute of Engineering · BRUniversidade Federal de Minas Gerais · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

DNA topoisomerase I from Plasmodium falciparum (PfTopoI), a potential selective target for chemotherapy and drug development against malaria, is used here, together with human Topo I (HssTopoI), for docking, molecular dynamics (MD) studies and experimental assays. Six synthetic isoflavonoid derivatives and the known PfTopoI inhibitors camptothecin and topotecan were evaluated in parallel. Theoretical results suggest that these compounds dock in the binding site of camptothecin and topotecan inside both enzymes and that LQB223 binds selectively in PfTopoI. In vitro tests against P. falciparum blood parasites corroborated the theoretical findings. The selectivity index (SI) of LQB223 ≥ 98 suggests that this molecule is the most promising in the group of compounds tested. In vivo experiments in mice infected with P. berghei showed that LQB223 has an antimalarial activity similar to that of chloroquine.

Indexed as

AnimalsAntimalarialsCamptothecinCrystallography, X-RayDNA Topoisomerases, Type IDose-Response Relationship, DrugDrug ResistanceFemaleHumansInhibitory Concentration 50IsoflavonesMalaria, FalciparumMiceMolecular Docking SimulationMolecular Dynamics SimulationParasitesAntimalarialsCamptothecinDNA Topoisomerases, Type IIsoflavonesTopoisomerase InhibitorsTopotecan

Identifiers

PMID24651068
PMCPMC3961230
OpenAlexW2046741242

What OpenQuestion holds

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LicenceCC BY
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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.