Evidence map›Paper›PMID 34933639›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2022

Polycyclic nitrogen heterocycles as potential thymidine phosphorylase inhibitors: synthesis, biological evaluation, and molecular docking study.

Karen Aknin, Alexis Bontemps, Amaury Farce, Eric Merlet, Philippe Belmont, Philippe Helissey, Philippe Chavatte, Marie-Agnès Sari, Sylviane Giorgi-Renault, Stéphanie Desbène-Finck

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2022. 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. Review
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.

Karen AkninFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Alexis BontempsFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Amaury FarceInserm, CHU Lille, U1286 - INFINITE - Institute for Translational Research in Inflammation, Université de Lille, Lille, France.
Eric MerletFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Philippe BelmontFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Philippe HelisseyFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Philippe ChavatteInserm, CHU Lille, U1286 - INFINITE - Institute for Translational Research in Inflammation, Université de Lille, Lille, France.
Marie-Agnès SariFaculté des Sciences, CNRS, UMR 8601, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, Université de Paris, Paris, France.
Sylviane Giorgi-RenaultFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.
Stéphanie Desbène-FinckFaculté de Santé, Faculté de Pharmacie de Paris, Cibles Thérapeutiques et Conception de Médicaments (CiTCoM), CNRS UMR8038, Université de Paris, Paris, France.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

New polycyclic heterocycles were synthesised and evaluated as potential inhibitors of thymidine phosphorylase (TP). Inspired by the pharmacophoric pyrimidinedione core of the natural substrate, four series have been designed in order to interact with large empty pockets of the active site: pyrimidoquinoline-2,4-diones (series A), pyrimidinedione linked to a pyrroloquinoline-1,3-diones (series B and C), the polycyclic heterocycle has been replaced by a pyrimidopyridopyrrolidinetetraone (series D). In each series, the tricyclic nitrogen heterocyclic moiety has been synthesised by a one-pot multicomponent reaction. Compared to

Indexed as

Molecular Docking SimulationCell LineCell SurvivalDose-Response Relationship, DrugEnzyme InhibitorsHeterocyclic CompoundsHumansMolecular StructureNitrogenPolycyclic CompoundsStructure-Activity RelationshipThymidine PhosphorylaseEnzyme InhibitorsHeterocyclic CompoundsNitrogenPolycyclic CompoundsThymidine PhosphorylaseTYMP protein, humanmolecular dockingmulticomponent reactionspyrido[2,3-d]pyrimidinedionepyrimido[4,5-b]quinoline-2,4-dioneThymidine phosphorylase inhibitor

Identifiers

PMID34933639
PMCPMC8725971

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.