Evidence map›Paper›PMID 40479895›Full record

ArticleEuropean journal of medicinal chemistry2025

Discovery of highly potent naphthalene/quinoline-based PAD inhibitors: Structure-activity relationship, selectivity, and cytotoxicity.

Yijiang Jia, Sina Bahraminejad, Xin Duan, Sydney Kong, Ayijiang Taledaohan, Chenyao Jiang, Dejian Ma, Jianxiong Jiang, Yuji Wang, Jiawang Liu

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European 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 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. 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

10 authors.

Yijiang JiaMedicinal Chemistry Core, Office of Research, University of Tennessee Health Science Center, Memphis, TN, 38163, USA; Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA.
Sina BahraminejadDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA.
Xin DuanDepartment of Neurology, Institute of Medicine, University of Tsukuba, Ibaraki, Japan.
Sydney KongCollege of Arts and Sciences, Vanderbilt University, Nashville, TN, 37240, USA.
Ayijiang TaledaohanDepartment of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You an Men, Beijing, 100069, PR China; Department of Medicinal Chemistry, Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Beijing Laboratory of Biomedical Materials, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, 10 Xi Tou Tiao, You an Men, Beijing, 100069, PR China.
Chenyao JiangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA.
Dejian MaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA.
Jianxiong JiangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA.
Yuji WangDepartment of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You an Men, Beijing, 100069, PR China; Department of Medicinal Chemistry, Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Beijing Laboratory of Biomedical Materials, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, 10 Xi Tou Tiao, You an Men, Beijing, 100069, PR China. Electronic address: wangyuji@ccmu.edu.cn.
Jiawang LiuMedicinal Chemistry Core, Office of Research, University of Tennessee Health Science Center, Memphis, TN, 38163, USA; Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN, 38163, USA. Electronic address: jliu90@uthsc.edu.

Funding

Trans-omics Integration of Multi-omics Studies for OsteoporosisU19AG055373 · NIA · TULANE UNIVERSITY OF LOUISIANA · PI Chuan Qiu · 2017 to 2026
$24.3M
EP2 Antagonists for Ischemic StrokeR61NS130199 · NINDS · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI JIANG, JIANXIONG, LIU, JIAWANG · 2023 to 2024
$752k
Acquisition of a Q-TOF Mass SpectrometerS10OD010678 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2012 to 2012
$325k
Mass Spectrometer for Small Molecule Drug DevelopmentS10OD016226 · OD · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI MEIBOHM, BERND · 2014 to 2014
$316k
Acquisition of a 400MHz Solution NMR System with an AutosamplerS10RR026377 · NCRR · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI · 2010 to 2010
$253k
NCRR NIH HHS S10 RR026377NIA NIH HHS U19 AG055373NIH HHS S10 OD010678NIH HHS S10 OD016226NINDS NIH HHS R61 NS130199
6 · The paper itself

Abstract

This study focuses on developing highly potent inhibitors targeting peptidyl arginine deiminases (PADs), particularly PAD4 and PAD1, which play critical roles in citrullination-linked diseases such as cancer and autoimmune disorders. A series of benzylamine- and benzimidazole-substituted compounds were synthesized and evaluated for their inhibitory activity. Key findings include the identification of naphthalene and quinoline-based scaffolds with hydroxyl substitutions, which exhibited superior inhibition of PAD1 and PAD4 (IC

Indexed as

Drug DiscoveryEnzyme InhibitorsNaphthalenesQuinolinesCell ProliferationDose-Response Relationship, DrugHumansMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipEnzyme InhibitorsnaphthaleneNaphthalenesquinolineQuinolinesCitrullinationEnzyme inhibitionNaphthalene scaffoldPAD inhibitorStructure-activity relationship

Identifiers

PMID40479895
PMCPMC12477756

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.