Evidence map›Paper›PMID 29271659›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2018

Small molecule purine and pseudopurine derivatives: synthesis, cytostatic evaluations and investigation of growth inhibitory effect in non-small cell lung cancer A549.

Andrea Bistrović, Petra Grbčić, Anja Harej, Mirela Sedić, Sandra Kraljević-Pavelić, Sanja Koštrun, Janez Plavec, Damjan Makuc, Silvana Raić-Malić

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2018. 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
1.7field-weighted citation impact, top 15% 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, 26 citations in OpenAlex.

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  6. Enhanced expression of queuine tRNA-ribosyltransferase 1 (Annals of translational medicine · 2020
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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 2 countries.

Andrea Bistrovića Department of Organic Chemistry, Faculty of Chemical Engineering and Technology , University of Zagreb , Zagreb , Croatia.
Petra Grbčićb Department of Biotechnology, Center for High-Throughput Technologies , University of Rijeka , Rijeka , Croatia.
Anja Harejb Department of Biotechnology, Center for High-Throughput Technologies , University of Rijeka , Rijeka , Croatia.
Mirela Sedićb Department of Biotechnology, Center for High-Throughput Technologies , University of Rijeka , Rijeka , Croatia.
Sandra Kraljević-Pavelićb Department of Biotechnology, Center for High-Throughput Technologies , University of Rijeka , Rijeka , Croatia.
Sanja Koštrunc Chemistry Department , Fidelta Ltd. , Zagreb , Croatia.
Janez Plavecd Slovenian NMR Centre , National Institute of Chemistry , Ljubljana , Slovenia.
Damjan Makucd Slovenian NMR Centre , National Institute of Chemistry , Ljubljana , Slovenia.
Silvana Raić-Malića Department of Organic Chemistry, Faculty of Chemical Engineering and Technology , University of Zagreb , Zagreb , Croatia.
University of Rijeka · HREN-FIST Centre of Excellence (Slovenia) · SIUniversity of Zagreb · HRPliva (Croatia) · HR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Novel halogenated purines and pseudopurines with diverse aryl-substituted 1,2,3-triazoles were prepared. While p-(trifluoromethyl)-substituted 1,2,3-triazole in N-9 alkylated purine and 3-deazapurine was critical for strong albeit unselective activity on pancreatic adenocarcinoma cells CFPAC-1,1-(p-fluorophenyl)-1,2,3-triazole derivative of 7-deazapurine showed selective cytostatic effect on metastatic colon cancer cells SW620. Importantly, 1-(p-chlorophenyl)-1,2,3-triazole-tagged benzimidazole displayed the most pronounced and highly selective inhibitory effect in nM range on non-small cell lung cancer A549. This compound revealed to target molecular processes at the extracellular side and inside the plasma membrane regulated by GPLD1 and growth factor receptors PDGFR and IGF-1R leading to the inhibition of cell proliferation and induction of apoptosis mediated by p38 MAP kinase and NF-κB, respectively. Further optimisation of this compound as to reduce its toxicity in normal cells may lead to the development of novel agent effective against lung cancer.

Indexed as

Antineoplastic AgentsApoptosisCarcinoma, Non-Small-Cell LungCell ProliferationCells, CulturedCytostatic AgentsDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansLung NeoplasmsModels, MolecularMolecular StructurePurinesSmall Molecule LibrariesStructure-Activity RelationshipTriazolesAntineoplastic AgentsCytostatic AgentsPurinesSmall Molecule LibrariesTriazoles1,2,3-triazolenon-small cell lung cancer A549p38 MAPKPurinepurinomimetic

Identifiers

PMID29271659
PMCPMC6009932
OpenAlexW2774124136

What OpenQuestion holds

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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.