Evidence map›Paper›PMID 34073771›Full record

ArticleMolecules (Basel, Switzerland)2021

Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments.

Aldar A Munkuev, Evgenii S Mozhaitsev, Arina A Chepanova, Evgeniy V Suslov, Dina V Korchagina, Olga D Zakharova, Ekaterina S Ilina, Nadezhda S Dyrkheeva, Alexandra L Zakharenko, Jóhannes Reynisson and 3 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.5field-weighted citation impact, top 17% 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

13 citing papers in PubMed, 26 citations in OpenAlex.

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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

13 authors at 3 institutions in 2 countries.

Aldar A MunkuevN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.ORCID 0000-0002-1504-5880
Evgenii S MozhaitsevN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.
Arina A ChepanovaInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.
Evgeniy V SuslovN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.ORCID 0000-0003-0988-0502
Dina V KorchaginaN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.
Olga D ZakharovaInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.
Ekaterina S IlinaInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.
Nadezhda S DyrkheevaInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.
Alexandra L ZakharenkoInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.
Jóhannes ReynissonSchool of Pharmacy and Bioengineering, Keele University, Hornbeam Building, Staffordshire ST5 5BG, UK.ORCID 0000-0003-4174-9512
Konstantin P VolchoN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.ORCID 0000-0002-4083-9324
Nariman F SalakhutdinovN. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9, Akademika Lavrentieva Ave., 630090 Novosibirsk, Russia.
Olga I LavrikInstitute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Sciences, 8, Lavrentiev Ave., 630090 Novosibirsk, Russia.ORCID 0000-0001-5980-8889
Institute of Chemical Biology and Fundamental Medicine · RUNovosibirsk Institute of Organic Chemistry · RUKeele University · GB

Funding

Russian Scientific Foundation 19-13-00040
6 · The paper itself

Abstract

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising target for anticancer therapy due to its ability to counter the effects topoisomerase 1 (Top1) poison, such as topotecan, thus, decreasing their efficacy. Compounds containing adamantane and monoterpenoid residues connected via 1,2,4-triazole or 1,3,4-thiadiazole linkers were synthesized and tested against Tdp1. All the derivatives exhibited inhibition at low micromolar or nanomolar concentrations with the most potent inhibitors having IC

Indexed as

AdamantaneCarbon-13 Magnetic Resonance SpectroscopyCell Line, TumorHumansLigandsMass SpectrometryMonoterpenesPhosphoric Diester HydrolasesProton Magnetic Resonance SpectroscopyStructure-Activity RelationshipAdamantaneLigandsMonoterpenesPhosphoric Diester HydrolasesTDP1 protein, humancancerchemical spaceDNA repair enzymemolecular modelingmonoterpenoidSARtopoisomerase 1

Identifiers

PMID34073771
PMCPMC8197275
OpenAlexW3165643857

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.