Evidence map›Paper›PMID 41110127›Full record

ArticleJournal of medicinal chemistry2025

Development of Selective and Soluble Mitochondrial Complex 1 Inhibitors Derived from Papaverine for Radiosensitization of Cancer.

Ben J Haines, McKenzie Kreamer, Martin Benej, Shabber Mohammed, Haylee Bridge, Esin Bayrali-Ulker, Adel Fergatova, Terence M Williams, Zihai Li, Ioanna Papandreou and 2 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. 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

12 authors.

Ben J HainesDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
McKenzie KreamerDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Martin BenejDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Shabber MohammedDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
Haylee BridgeDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
Esin Bayrali-UlkerDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Adel FergatovaDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Terence M WilliamsDepartment of Radiation Oncology, City of Hope National Medical Center, Duarte, California 91010, United States.ORCID 0000-0002-1020-0845
Zihai LiPelotonia Institute for Immuno-Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Ioanna PapandreouDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.
Nicholas C DenkoDepartment of Radiation Oncology, The Ohio State University Comprehensive Cancer Center, College of Medicine, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210, United States.ORCID 0000-0001-6875-734X
Mark J Mitton-FryDivision of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.ORCID 0000-0002-6715-8836

Funding

Overcoming Hypoxic Resistance in Non-Small Cell Lung Cancer By Targeting Mitochondrial MetabolismR01CA262388 · NCI · OHIO STATE UNIVERSITY · PI DENKO, NICHOLAS C., LI, ZIHAI · 2021 to 2025
$3.6M
Overcoming hypoxic resistance to anti-cancer therapyR01CA255334 · NCI · OHIO STATE UNIVERSITY · PI DENKO, NICHOLAS C., LI, ZIHAI · 2021 to 2025
$2.9M
NCI NIH HHS R01 CA255334NCI NIH HHS R01 CA262388
6 · The paper itself

Abstract

The efficacy of radiation therapy is limited by low oxygen tension within solid tumors. Papaverine and some derivatives were previously shown to inhibit mitochondrial complex 1 and decrease oxygen consumption, reversing hypoxia and radiosensitizing model tumors. Papaverine is typically used as a vasorelaxant due to its ability to inhibit phosphodiesterase 10A (PDE10A), which can lead to unwanted side effects when used clinically as a radiosensitizer. We have therefore generated additional derivatives which have improved mitochondrial complex 1 inhibition and reduced PDE10A inhibition. Two of these compounds were tested

Indexed as

Electron Transport Complex IPapaverineRadiation-Sensitizing AgentsAnimalsCell Line, TumorFemaleHumansMammary Neoplasms, ExperimentalMiceSolubilityStructure-Activity RelationshipElectron Transport Complex IPapaverineRadiation-Sensitizing Agents

Identifiers

PMID41110127
PMCPMC12621195

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.