Evidence map›Paper›PMID 38875806›Full record

ArticleEuropean journal of medicinal chemistry2024

Evaluation of potency and metabolic stability of diphyllin-derived Vacuolar-ATPase inhibitors.

Laura M Sanford, Patrick Keiser, Naoaki Fujii, Hannah Woods, Charlie Zhang, Zhuangyan Xu, Nivedita S Mahajani, Julián González Cortés, Caroline B Plescia, Gregory Knipp and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
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.

Laura M SanfordBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Patrick KeiserDepartment of Microbiology, National Emerging Infectious Diseases Laboratories, Boston University, Boston, MA, 02118, United States.
Naoaki FujiiBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Hannah WoodsBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Charlie ZhangBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States; Department of Industrial and Molecular Pharmaceutics, Purdue University, West Lafayette, IN, 47907, United States.
Zhuangyan XuDepartment of Industrial and Molecular Pharmaceutics, Purdue University, West Lafayette, IN, 47907, United States.
Nivedita S MahajaniBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Julián González CortésBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Caroline B PlesciaBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Gregory KnippDepartment of Industrial and Molecular Pharmaceutics, Purdue University, West Lafayette, IN, 47907, United States.
Robert V StahelinBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States.
Robert DaveyDepartment of Microbiology, National Emerging Infectious Diseases Laboratories, Boston University, Boston, MA, 02118, United States.
Vincent Jo DavissonBorch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, United States. Electronic address: davisson@purdue.edu.

Funding

Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI ANDREW D MESECAR · 1985 to 2026
$43.4M
Antiviral Lead Identification to Treat Filovirus InfectionsR01AI128364 · NIAID · PURDUE UNIVERSITY · PI DAVEY, ROBERT A, DAVISSON, VINCENT JO · 2019 to 2022
$2.6M
NCI NIH HHS P30 CA023168NIAID NIH HHS R01 AI128364
6 · The paper itself

Abstract

Diphyllin is a naturally occurring lignan comprised of an aryl naphthalene lactone scaffold that demonstrates beneficial biological activities in disease models of cancer, obesity, and viral infection. A target of diphyllin and naturally occurring derivatives is the vacuolar ATPase (V-ATPase) complex. Although diphyllin-related natural products are active with in vitro models for viral entry, the potencies and unknown pharmacokinetic properties limit well-designed in vivo evaluations. Previous studies demonstrated that diphyllin derivatives have the utility of blocking the Ebola virus cell entry pathway. However, diphyllin shows limited potency and poor oral bioavailability in mice. An avenue to improve the potency was used in a new library of synthetic derivatives of diphyllin. Diphyllin derivatives exploiting ether linkages at the 4-position with one-to-three carbon spacers to an oxygen or nitrogen atom provided compounds with EC

Indexed as

Antiviral AgentsVacuolar Proton-Translocating ATPasesAnimalsDose-Response Relationship, DrugEbolavirusEnzyme InhibitorsHumansLignansMiceMolecular StructureNaphthalenesStructure-Activity RelationshipVirus InternalizationAntiviral AgentsdiphyllinEnzyme InhibitorsLignansNaphthalenesVacuolar Proton-Translocating ATPasesAntiviralDiphyllinEbola virusNatural productPharmacokinetics

Identifiers

PMID38875806
PMCPMC11236507

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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.