ArticleBioorganic & medicinal chemistry letters2016
Indole-based allosteric inhibitors of HIV-1 integrase.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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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.
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Who cites it
18 citing papers in PubMed, 31 citations in OpenAlex.
- Mapping the TAR vRNA Interaction with HIV-1 Integrase.Viruses · 2026Article
- Mapping the vRNA Interaction with HIV-1 Integrase.bioRxiv : the preprint server for biology · 2026Article
- Carbon-Atom Scavengers Enable Divergent, Selective Carbon Deletion of Azaarenes.Journal of the American Chemical Society · 2025Article
- Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as novel HIV-1 integrase strand transfer inhibitors.RSC advances · 2024Article
- Optimizing the Multimerization Properties of Quinoline-Based Allosteric HIV-1 Integrase Inhibitors.Viruses · 2024Review
- Dihydroxyphenyl- and Heteroaromatic-Based Thienopyrimidinones to Tackle HIV-1 LEDGF/p75-Dependent IN Activity.Molecules (Basel, Switzerland) · 2023Article
- Regioselective synthesis of 3-nitroindoles under non-acidic and non-metallic conditions.RSC advances · 2023Article
- Structure of a HIV-1 IN-Allosteric inhibitor complex at 2.93 Å resolution: Routes to inhibitor optimization.PLoS pathogens · 2023Article
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- Fecal Metabolome Signature in the HIV-1 Elite Control Phenotype: Enrichment of Dipeptides Acts as an HIV-1 Antagonist but aJournal of virology · 2021Article
- A highly potent and safe pyrrolopyridine-based allosteric HIV-1 integrase inhibitor targeting host LEDGF/p75-integrase interaction site.PLoS pathogens · 2021Article
- Retroviral integrase: Structure, mechanism, and inhibition.The Enzymes · 2021Article
- HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors.eLife · 2019Article
- New targets for HIV drug discovery.Drug discovery today · 2019Review
- An Isoquinoline Scaffold as a Novel Class of Allosteric HIV-1 Integrase Inhibitors.ACS medicinal chemistry letters · 2019Article
- Synthesis and Evaluation of Aryl Quinolines as HIV-1 Integrase Multimerization Inhibitors.ACS medicinal chemistry letters · 2018Article
- Optimized binding of substituted quinoline ALLINIs within the HIV-1 integrase oligomer.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
Abstract
Employing a scaffold hopping approach, a series of allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) have been synthesized based on an indole scaffold. These compounds incorporate the key elements utilized in quinoline-based ALLINIs for binding to the IN dimer interface at the principal LEDGF/p75 binding pocket. The most potent of these compounds displayed good activity in the LEDGF/p75 dependent integration assay (IC50=4.5μM) and, as predicted based on the geometry of the five- versus six-membered ring, retained activity against the A128T IN mutant that confers resistance to many quinoline-based ALLINIs.
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Registered trials
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.