Evidence map›Paper›PMID 42511764›Full record

ArticleInternational journal of molecular sciences2026

Synthesis and Biological Evaluation of TDP1 Inhibitors Based on Coumarin and Monoterpenoid Fragments Conjoined by Heterocyclic Moieties.

Dmitriy Tsypyshev, Tatyana Khomenko, Tatyana Kornienko, Alexandra Zakharenko, Nina Komarova, Vyacheslav Krasnov, Natalya Soldatova, Pavel Postnikov, Suat Sari, Konstantin Volcho and 2 more

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Article in International journal of molecular sciences, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed
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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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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.

Dmitriy TsypyshevNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.
Tatyana KhomenkoNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0009-0007-5702-3595
Tatyana KornienkoInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0000-0002-5427-9786
Alexandra ZakharenkoInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.
Nina KomarovaNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.
Vyacheslav KrasnovNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0000-0002-5387-8365
Natalya SoldatovaTomsk Polytechnic University, Tomsk 634050, Russia.
Pavel PostnikovNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0000-0001-9713-1290
Suat SariDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara 06230, Turkey.ORCID 0000-0002-8248-4218
Konstantin VolchoNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0000-0002-4083-9324
Olga LavrikInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.ORCID 0000-0001-5980-8889
Nariman SalakhutdinovNovosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences (SB RAS), Novosibirsk 630090, Russia.

Funding

Russian Science Foundation 25-73-20089
6 · The paper itself

Abstract

Tyrosyl-DNA phosphodiesterase 1 (TDP1) represents a compelling pharmacological target for the development of agents designed to circumvent tumor resistance to topoisomerase 1 (TOP1) inhibitors, a major class of clinically relevant antineoplastic drugs. This paper describes the design and synthesis of novel hybrid TDP1 inhibitors combining coumarin and monoterpene moieties via rigid isoxazole and 1,2,3-triazole heterocyclic linkers. The synthesis was accomplished via [3 + 2] cycloaddition of nitrile oxides to alkynes and copper-catalyzed click chemistry. Biological tests have demonstrated the crucial role of linker nature in the activity of the compounds. Isoxazole-linked conjugates showed strong inhibitory effects on TDP1, with IC

Indexed as

CoumarinsHeterocyclic CompoundsMonoterpenesPhosphodiesterase InhibitorsPhosphoric Diester HydrolasesAntineoplastic AgentsHeLa CellsHumansStructure-Activity RelationshipAntineoplastic AgentscoumarinCoumarinsHeterocyclic CompoundsMonoterpenesPhosphodiesterase InhibitorsPhosphoric Diester HydrolasesTDP1 protein, humancancercoumarinDNA repairenzyme inhibitionheterocyclesmonoterpenesynergy

Identifiers

PMID42511764
PMCPMC13409999

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Registered trials

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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.