Evidence map›Paper›PMID 32066010›Full record

ArticleEuropean journal of medicinal chemistry2020

Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities.

Lin Sun, Tianguang Huang, Alexej Dick, Megan E Meuser, Waleed A Zalloum, Chin-Ho Chen, Xiao Ding, Ping Gao, Simon Cocklin, Kuo-Hsiung Lee and 2 more

Abstract read
In one paragraph

Article in European 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 33 papers.

0numbers the graph read from it
0cells of the map it votes in
33citing 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

33 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Review
  6. Review
  7. Article
  8. Molecules (Basel, Switzerland) · 2024
    Review
  9. Article
  10. Article
  11. Review
  12. Recent Advances in the Green Synthesis of ActivePharmaceuticals (Basel, Switzerland) · 2023
    Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Silver-Catalyzed Cascade Cyclization of Amino-Molecules (Basel, Switzerland) · 2022
    Article
  18. Article
  19. Article
  20. GANAB andInternational journal of molecular sciences · 2022
    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

12 authors.

Lin SunDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.
Tianguang HuangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.
Alexej DickDepartment of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA.
Megan E MeuserDepartment of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA.
Waleed A ZalloumDepartment of Pharmacy, Faculty of Health Science, American University of Madaba, P.O Box 2882, Amman, 11821, Jordan.
Chin-Ho ChenDuke University Medical Center, Box 2926, Surgical Oncology Research Facility, Durham, NC, 27710, USA.
Xiao DingDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.
Ping GaoDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China.
Simon CocklinDepartment of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA, USA. Electronic address: sc349@drexel.edu.
Kuo-Hsiung LeeNatural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599, USA. Electronic address: khlee@unc.edu.
Peng ZhanDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China. Electronic address: zhanpeng1982@sdu.edu.cn.
Xinyong LiuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Ji'nan, Shandong, PR China. Electronic address: xinyongl@sdu.edu.cn.

Funding

Interdisciplinary And Translational Research Training In NeurohivT32MH079785 · NIMH · TEMPLE UNIV OF THE COMMONWEALTH · PI Kamel Khalili · 2008 to 2026
$5.4M
Novel anti-HIV compounds targeting the HIV-1 matrix proteinR01AI150491 · NIAID · DREXEL UNIVERSITY · PI LOLL, PATRICK J · 2020 to 2022
$1.7M
Novel anti-HIV compounds targeting the HIV-1 matrix proteinR01GM125396 · NIGMS · DREXEL UNIVERSITY · PI COCKLIN, SIMON · 2018 to 2019
$1.1M
NIAID NIH HHS R01 AI150491NIGMS NIH HHS R01 GM125396NIMH NIH HHS T32 MH079785
6 · The paper itself

Abstract

HIV-1 CA is involved in different stages of the viral replication cycle, performing essential roles in both early (uncoating, reverse transcription, nuclear import, integration) and late events (assembly). Recent efforts have demonstrated HIV-1 CA protein as a prospective therapeutic target for the development of new antivirals. The most extensively studied CA inhibitor, PF-3450074 (PF-74, discovered by Pfizer), that targets an inter-protomer pocket within the CA hexamer. Herein we reported the design, synthesis, and biological evaluation of a series of 4-phenyl-1H-1,2,3-triazole phenylalanine derivatives as HIV-1 CA inhibitors based on PF-74 scaffold. Most of the analogues demonstrated potent antiviral activities, among them, the anti-HIV-1 activity of 6a-9 (EC

Indexed as

Anti-HIV AgentsCapsid ProteinsCell Line, TumorDrug DesignHIV-1HumansMicrobial Sensitivity TestsMicrosomes, LiverMolecular Dynamics SimulationMolecular StructurePhenylalanineProtein BindingStructure-Activity RelationshipTriazolesVirus ReplicationAnti-HIV AgentsCapsid ProteinsPhenylalanineTriazoles1,2,3-TriazoleCA proteinHIV-1MD simulationPhenylalanine derivativesSPR assay

Identifiers

PMID32066010
PMCPMC7053825

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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.