Evidence map›Paper›PMID 33734714›Full record

ArticleJournal of medicinal chemistry2021

2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.

Dongwei Kang, Francesc X Ruiz, Yanying Sun, Da Feng, Lanlan Jing, Zhao Wang, Tao Zhang, Shenghua Gao, Lin Sun, Erik De Clercq and 4 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing 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

11 citing papers in PubMed.

  1. Review
  2. Article
  3. Recent Advances in Pyrimidine-Based Drugs.Pharmaceuticals (Basel, Switzerland) · 2024
    Review
  4. Article
  5. Article
  6. Article
  7. Journal of medicinal chemistry · 2023
    Article
  8. Article
  9. Article
  10. Article
  11. 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

14 authors.

Dongwei KangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.ORCID 0000-0001-9232-953X
Francesc X RuizCenter for Advanced Biotechnology and Medicine, Rutgers University, Piscataway, New Jersey 08854, United States.
Yanying SunDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Da FengDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Lanlan JingDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Zhao WangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Tao ZhangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Shenghua GaoDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.
Lin SunDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.ORCID 0000-0002-8395-5886
Erik De ClercqRega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Katholieke Universiteit Leuven, Herestraat 49 Postbus 1043 (09.A097), Leuven B-3000, Belgium.ORCID 0000-0002-2985-8890
Christophe PannecouqueRega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Katholieke Universiteit Leuven, Herestraat 49 Postbus 1043 (09.A097), Leuven B-3000, Belgium.
Eddy ArnoldCenter for Advanced Biotechnology and Medicine, Rutgers University, Piscataway, New Jersey 08854, United States.ORCID 0000-0003-2612-9622
Peng ZhanDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.ORCID 0000-0002-9675-6026
Xinyong LiuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, Jinan 250012, Shandong, PR China.ORCID 0000-0002-7302-2214

Funding

STRUCTURES OF HIV REVERSE TRANSCRIPTASE WITH SUBSTRATESR37AI027690 · NIAID · RUTGERS THE ST UNIV OF NJ NEW BRUNSWICK · PI ARNOLD, EDWARD · 1999 to 2018
$14.4M
STRUCTURES OF HIV REVERSE TRANSCRIPTASE WITH SUBSTRATESR01AI027690 · NIAID · UNIV OF MED/DENT NJ-R W JOHNSON MED SCH · PI EDWARD ARNOLD · 1989 to 2026
$4.3M
NIAID NIH HHS R01 AI027690NIAID NIH HHS R37 AI027690
6 · The paper itself

Abstract

There is an urgent unmet medical need for novel human immunodeficiency virus type 1 (HIV-1) inhibitors that are effective against a variety of NNRTI-resistance mutations. We report our research efforts aimed at discovering a novel chemotype of anti-HIV-1 agents with improved potency against a variety of NNRTI-resistance mutations in this paper. Structural modifications of the lead

Indexed as

AnimalsAnti-HIV AgentsCrystallography, X-RayDrug DesignHEK293 CellsHIV-1HIV Reverse TranscriptaseHumansMiceMicrobial Sensitivity TestsMolecular StructureMutationProtein BindingPyrimidinesRatsRats, Sprague-DawleyAnti-HIV AgentsHIV Reverse TranscriptasePyrimidinesReverse Transcriptase Inhibitors

Identifiers

PMID33734714
PMCPMC8594587

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.