Evidence map›Paper›PMID 33079544›Full record

ArticleJournal of medicinal chemistry2020

Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β.

Jose Antonio Ortega, Jose M Arencibia, Elirosa Minniti, Jo Ann W Byl, Sebastian Franco-Ulloa, Marco Borgogno, Vito Genna, Maria Summa, Sine Mandrup Bertozzi, Rosalia Bertorelli and 5 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.3field-weighted citation impact, top 19% 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

11 citing papers in PubMed, 29 citations in OpenAlex.

  1. Review
  2. SAR exploration for 4-aminotetrahydroquinazolines with adamantyl moiety against orthoflaviviruses.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
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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

15 authors at 4 institutions in 2 countries.

Jose Antonio OrtegaLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Jose M ArencibiaLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Elirosa MinnitiLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Jo Ann W BylDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146, United States.
Sebastian Franco-UlloaLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.ORCID 0000-0001-6128-0630
Marco BorgognoLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Vito GennaLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.ORCID 0000-0002-4664-8086
Maria SummaAnalytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Sine Mandrup BertozziAnalytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Rosalia BertorelliAnalytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.
Andrea ArmirottiAnalytical Chemistry & Translational Pharmacology, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.ORCID 0000-0002-3766-8755
Anna MinariniDepartment of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Claudia SissiDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo 5, 35131 Padova, Italy.ORCID 0000-0002-9713-1415
Neil OsheroffDepartment of Biochemistry, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0002-2550-4884
Marco De VivoLaboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy.ORCID 0000-0003-4022-5661
Italian Institute of Technology · ITVanderbilt University · USUniversity of Bologna · ITUniversity of Padua · IT

Funding

Mechanistic Studies of Type II Topoisomerases and Topoisomerase-Targeted AgentsR01GM126363 · NIGMS · VANDERBILT UNIVERSITY · PI OSHEROFF, NEIL · 2018 to 2025
$2.6M
NIGMS NIH HHS R01 GM126363
6 · The paper itself

Abstract

We disclose a novel class of 6-amino-tetrahydroquinazoline derivatives that inhibit human topoisomerase II (topoII), a validated target of anticancer drugs. In contrast to topoII-targeted drugs currently in clinical use, these compounds do not act as topoII poisons that enhance enzyme-mediated DNA cleavage, a mechanism that is linked to the development of secondary leukemias. Instead, these tetrahydroquinazolines block the topoII function with no evidence of DNA intercalation. We identified a potent lead compound [compound

Indexed as

AnimalsCell Line, TumorCell SurvivalDNADNA CleavageDNA Topoisomerases, Type IIDrug Screening Assays, AntitumorHalf-LifeHumansIsoenzymesMiceQuinidineTopoisomerase II InhibitorsDNADNA Topoisomerases, Type IIhydroquinidineIsoenzymesQuinidineTopoisomerase II Inhibitors

Identifiers

PMID33079544
PMCPMC7668297
OpenAlexW3094092853

What OpenQuestion holds

Textmetadata
LicenceTDM
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.