Evidence map›Paper›PMID 41455111›Full record

ArticleJournal of medicinal chemistry2026

Discovery of Fused Isoquinolinone/Triazole as a Scaffold for Tankyrase and PARP Inhibition.

Konstantinos A Ouzounthanasis, Chiara Bosetti, Juho Alaviuhkola, Saurabh S Dhakar, Christiana Mantzourani, Maroula G Kokotou, Demetrios Kanetidis, Lari Lehtiö, Alexandros E Koumbis

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Article in Journal of medicinal chemistry, 2026. 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

9 authors.

Konstantinos A OuzounthanasisLaboratory of Organic Chemistry, Department of Chemistry, Aristotle University, 54124 Thessaloniki, Greece.
Chiara BosettiFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, 90220 Oulu, Finland.
Juho AlaviuhkolaFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, 90220 Oulu, Finland.
Saurabh S DhakarFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, 90220 Oulu, Finland.
Christiana MantzouraniLaboratory of Chemistry, Department of Food Science and Human Nutrition, Agricultural University of Athens, 11855 Athens, Greece.ORCID 0000-0002-2621-1231
Maroula G KokotouLaboratory of Chemistry, Department of Food Science and Human Nutrition, Agricultural University of Athens, 11855 Athens, Greece.
Demetrios KanetidisLaboratory of Organic Chemistry, Department of Chemistry, Aristotle University, 54124 Thessaloniki, Greece.
Lari LehtiöFaculty of Biochemistry and Molecular Medicine & Biocenter Oulu, University of Oulu, 90220 Oulu, Finland.ORCID 0000-0001-7250-832X
Alexandros E KoumbisLaboratory of Organic Chemistry, Department of Chemistry, Aristotle University, 54124 Thessaloniki, Greece.ORCID 0000-0003-4391-7807

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A series of fused isoquinolinone/triazole hybrids were designed and prepared applying a unified versatile synthetic strategy. This practically involved three steps, a novel one-pot CuAAc "click" reaction-iodination process, an amidation and a copper-catalyzed intramolecular Ullmann cyclization and was found to be applicable for a variety of substitutions patterns on the main framework. Some of those synthesized hybrids were tested for selected ADP-ribosyltransferases and found to display nanomolar potency against TNKS2, whereas selectivity was also observed in comparison to other tested PARPs. The SAR studies divulged key structural features which are responsible for this selectivity. Moreover, the identification of the binding site of those selective derivatives using X-ray crystallography revealed that they are accommodated in the nicotinamide binding subsite while certain groups extend toward a hydrophobic pocket unique to tankyrases.

Indexed as

Enzyme InhibitorsIsoquinolinesPoly(ADP-ribose) Polymerase InhibitorsTankyrasesTriazolesCrystallography, X-RayDrug DiscoveryHumansModels, MolecularPoly(ADP-ribose) PolymerasesStructure-Activity RelationshipEnzyme InhibitorsIsoquinolinesPoly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesTankyrasesTriazoles

Identifiers

PMID41455111
PMCPMC12794163

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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.