Evidence map›Paper›PMID 37049762›Full record

ArticleMolecules (Basel, Switzerland)2023

Rational Design and Lead Optimisation of Potent Antimalarial Quinazolinediones and Their Cytotoxicity against MCF-7.

Sitthivut Charoensutthivarakul, Duangporn Lohawittayanan, Phongthon Kanjanasirirat, Kedchin Jearawuttanakul, Sawinee Seemakhan, Napason Chabang, Patrick Schlaeppi, Varisa Tantivess, Tanapol Limboonreung, Matthew Phanchana

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2023. 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
1.2field-weighted citation impact, top 25% 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, 8 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

10 authors at 2 institutions in 1 country.

Sitthivut CharoensutthivarakulInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.ORCID 0000-0002-4447-3438
Duangporn LohawittayananInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Phongthon KanjanasiriratExcellent Center for Drug Discovery, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.ORCID 0000-0002-1046-7152
Kedchin JearawuttanakulExcellent Center for Drug Discovery, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Sawinee SeemakhanExcellent Center for Drug Discovery, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Napason ChabangInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Patrick SchlaeppiInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Varisa TantivessInnovative Molecular Discovery Laboratory (iMoD), School of Bioinnovation and Bio-Based Product Intelligence, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Tanapol LimboonreungSchool of Dentistry, King Mongkut's Institute of Technology Ladkrabang, Bangkok 10520, Thailand.
Matthew PhanchanaDepartment of Molecular Tropical Medicine and Genetics, Faculty of Tropical Medicine, Mahidol University, Bangkok 10400, Thailand.ORCID 0000-0002-7736-7500
Mahidol University · THKing Mongkut's Institute of Technology Ladkrabang · TH

Funding

Mahidol University BRF1-A23/2564
6 · The paper itself

Abstract

Quinazolinedione is one of the most outstanding heterocycles in medicinal chemistry thanks to its wide ranges of biological activities including antimalarial, anticancer, and anti-inflammatory. TCMDC-125133 containing a quinazolinedione pharmacophore displays promising antimalarial activity and low toxicity, as described in the GlaxoSmithKline (GSK) report. Herein, the design and synthesis of novel quinazolinedione derivatives is described on the basis of our previous work on the synthesis of TCMDC-125133, where low-cost chemicals and greener alternatives were used when possible. The initial SAR study focused on the replacement of the valine linker moiety; according to the in silico prediction using SwissADME, concise four-step syntheses toward compounds

Indexed as

AntimalarialsHumansMCF-7 CellsPlasmodium falciparumStructure-Activity RelationshipAntimalarialsantimalarial activityantiproliferative activityquinazolinedione derivatives

Identifiers

PMID37049762
PMCPMC10096129
OpenAlexW4361221035

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.