Evidence map›Paper›PMID 25913935›Full record

ArticleMolecules (Basel, Switzerland)2015

Discovery of Metal Ions Chelator Quercetin Derivatives with Potent Anti-HCV Activities.

Dongwei Zhong, Mingming Liu, Yang Cao, Yelin Zhu, Shihui Bian, Jiayi Zhou, Fengjie Wu, Kum-Chol Ryu, Lu Zhou, Deyong Ye

Abstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Review
  6. Article
  7. Article
  8. Article
  9. Synthesis andAdvanced biomedical research · 2018
    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

10 authors.

Dongwei ZhongDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 12211030012@fudan.edu.cn.
Mingming LiuDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 09111030009@fudan.edu.cn.
Yang CaoDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 14111030010@fudan.edu.cn.
Yelin ZhuDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 09301030045@fudan.edu.cn.
Shihui BianDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 08301030057@fudan.edu.cn.
Jiayi ZhouDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 09301030009@fudan.edu.cn.
Fengjie WuDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. 11307120169@fudan.edu.cn.
Kum-Chol RyuInstitute of Pharmacy, HamHung Pharmaceutical University, HamHung 999093, Democratic People's Republic of Korea. yegroup@126.com.
Lu ZhouDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. zhoulu@fudan.edu.cn.
Deyong YeDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, 826 Zhang-Heng Rd, Shanghai 201203, China. dyye@shmu.edu.cn.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Analogues or isosteres of α,γ-diketoacid (DKA) 1a show potent inhibition of hepatitis C virus (HCV) NS5B polymerase through chelation of the two magnesium ions at the active site. The anti-HCV activity of the flavonoid quercetin (2) could partly be attributed to it being a structural mimic of DKAs. In order to delineate the structural features required for the inhibitory effect and improve the anti-HCV potency, two novel types of quercetin analogues, 7-O-arylmethylquercetins and quercetin-3-O-benzoic acid esters, were designed, synthesized and evaluated for their anti-HCV properties in cell-based assays. Among the 38 newly synthesized compounds, 7-O-substituted derivative 3i and 3-O-substituted derivative 4f were found to be the most active in the corresponding series (EC50 = 3.8 μM and 9.0 μΜ, respectively). Docking studies suggested that the quercetin analogues are capable of establishing key coordination with the two magnesium ions as well as interactions with residues at the active site of HCV NS5B.

Indexed as

Antiviral AgentsCatalytic DomainCell Line, TumorChelating AgentsDrug DiscoveryHepacivirusHumansMagnesiumModels, MolecularMolecular Docking SimulationMolecular StructureQuercetinRNA-Dependent RNA PolymeraseStructure-Activity RelationshipViral Nonstructural ProteinsAntiviral AgentsChelating AgentsMagnesiumNS-5 protein, hepatitis C virusQuercetinRNA-Dependent RNA PolymeraseViral Nonstructural Proteins

Identifiers

PMID25913935
PMCPMC6272327

What OpenQuestion holds

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Registered trials

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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.