Improving the positional adaptability: structure-based design of biphenyl-substituted diaryltriazines as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Kaijun Jin, Minjie Liu, Chunlin Zhuang, Erik De Clercq, Christophe Pannecouque, Ge Meng, Fener Chen

Abstract read

In one paragraph

Article in Acta pharmaceutica Sinica. B, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

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0cells of the map it votes in

7citing 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

7 citing papers in PubMed.

Drug Discovery and Exploration of Heterocycles for the Development of Anti-HIV Agents.Infectious disorders drug targets · 2025
Review
Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability.Acta pharmaceutica Sinica. B · 2023
Article
Approved HIV reverse transcriptase inhibitors in the past decade.Acta pharmaceutica Sinica. B · 2022
Review
In silico structural elucidation of the rabies RNA-dependent RNA polymerase (RdRp) toward the identification of potential rabies virus inhibitors.Journal of molecular modeling · 2021
Article
Antiviral and Antimicrobial Nucleoside Derivatives: Structural Features and Mechanisms of Action.Molecular biology · 2021
Article
Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years.Acta pharmaceutica Sinica. B · 2020
Review
Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy.Molecules (Basel, Switzerland) · 2020
Article

4 · The record

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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

7 authors.

Kaijun JinEngineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433 China.

Minjie LiuEngineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433 China.

Chunlin ZhuangEngineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433 China.

Erik De ClercqRega Institute for Medical Research, KU Leuven, Leuven B-3000 Belgium.

Christophe PannecouqueRega Institute for Medical Research, KU Leuven, Leuven B-3000 Belgium.

Ge MengEngineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433 China.

Fener ChenEngineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University, Shanghai 200433 China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

In order to improve the positional adaptability of our previously reported naphthyl diaryltriazines (NP-DATAs), synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is presented. These compounds exhibited excellent potency against wild-type (WT) HIV-1 with EC

Indexed as

AIDS, acquired immunodeficiency syndromeBP-DATA, biphenyl-substituted diaryltriazineBP-DATAsCC50, 50% cytotoxicity concentrationDAPY, diarylpyrimidineDATA, diaryltriazineEC50, the concentration causing 50% inhibition of antiviral activityEFV, efavirenzETR, etravirineHEPT, 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymineHIV-1HIV, human immunodeficiency virusMD, molecular dynamicMolecular modelingNNIBP, non-nucleoside inhibitor binding pocketNNRTI, non-nucleoside reverse transcriptase inhibitorNNRTIsNP-DATA, naphthyl diaryltriazineNP-DATAsNVP, nevirapinePK, pharmacokineticsPositional adaptabilityRMSD, root-mean square deviationRPV, rilpivirineRT, reverse transcriptaseSAR, structure–activity relationshipSI, selectivity indexTSAO, tert-butyldimethylsilyl-spiroaminooxathioledioxideWT, wild-type

Identifiers

PMID32082978

DOI10.1016/j.apsb.2019.09.007

PMCPMC7016291

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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.