Evidence map›Paper›PMID 40844434›Full record

ArticleChemMedChem2025

C1'-Branched Acyclic Nucleoside Phosphonates as Inhibitors of Plasmodium Falciparum 6-Oxopurine Phosphoribosyltransferase.

Jan Frydrych, Dianne T Keough, Haojun Xia, Lenka Poštová Slavětínská, Martin Dračínský, Michal Česnek, Jye Travis, Marina Chavchich, Michael Edstein, Dana Hocková and 2 more

Abstract read
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In one paragraph

Article in ChemMedChem, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. Article
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.

Jan FrydrychInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
Dianne T KeoughSchool of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, 4072, Australia.
Haojun XiaSchool of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, 4072, Australia.
Lenka Poštová SlavětínskáInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
Martin DračínskýInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
Michal ČesnekInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
Jye TravisDepartment of Drug Evaluation, Australian Defence Force Malaria and Infectious Disease Institute, Enoggera, Brisbane, Queensland, 4051, Australia.
Marina ChavchichDepartment of Drug Evaluation, Australian Defence Force Malaria and Infectious Disease Institute, Enoggera, Brisbane, Queensland, 4051, Australia.
Michael EdsteinDepartment of Drug Evaluation, Australian Defence Force Malaria and Infectious Disease Institute, Enoggera, Brisbane, Queensland, 4051, Australia.
Dana HockováInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.
Luke W GuddatSchool of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, 4072, Australia.ORCID https://orcid.org/0000-0002-8204-8408
Zlatko JanebaInstitute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, 160 00, Prague 6, Czech Republic.ORCID https://orcid.org/0000-0003-4654-679X

Funding

Institute of Organic Chemistry and Biochemistry RVO 61388963NHMRC 1030353
6 · The paper itself

Abstract

Hypoxanthine-guanine-(xanthine) phosphoribosyltransferase [HG(X)PRT] is an excellent target for the development of new drugs to treat parasitic and bacterial infections as well as MYC-dependent triple-negative breast cancer. Inhibitors include compounds that mimic the transition state of the catalytic reaction and analogs of the two products of the reaction, the nucleoside monophosphates and pyrophosphate. One type of chemistry explored here is the design of purine-based C1'-branched acyclic nucleoside phosphonates bearing diverse structural attachments (secondary linkers) on the C1' atom. Compounds where this secondary linker has either a terminal phosphonate or a hydroxyl group are submicromolar to single-digit micromolar inhibitors of human hypoxanthine-guanine phosphoribosyltransferase and Plasmodium falciparum HGXPRT. The lowest K

Indexed as

AntimalarialsEnzyme InhibitorsHypoxanthine PhosphoribosyltransferaseNucleosidesOrganophosphonatesPentosyltransferasesPlasmodium falciparumDose-Response Relationship, DrugHumansMolecular StructureStructure-Activity RelationshipAntimalarialsEnzyme Inhibitorshypoxanthine-guanine-xanthine phosphoribosyltransferaseHypoxanthine PhosphoribosyltransferaseNucleosidesOrganophosphonatesPentosyltransferasesacyclic nucleoside phosphonatesdockinghypoxanthine‐guanine‐(xanthine) phosphoribosyltransferaseinhibitorsmalariaPlasmodium falciparum

Identifiers

PMID40844434
PMCPMC12503909

What OpenQuestion holds

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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.