ArticleEuropean journal of medicinal chemistry2018
Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library.
Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 61 citations in OpenAlex.
- Click Chemistry Approach to Derivatisation of Fluconazole.Molecules (Basel, Switzerland) · 2026Article
- Understanding the HIV-CA protein and the ligands that bind at the N-terminal domain (NTD) - C-terminal domain (CTD) interface.RSC medicinal chemistry · 2025Review
- Design and Synthesis of New GS-6207 Subtypes for Targeting HIV-1 Capsid Protein.International journal of molecular sciences · 2024Article
- A Literature Review Focusing on the Antiviral Activity of [1,2,4] and [1,2,3]-triazoles.Mini reviews in medicinal chemistry · 2024Review
- Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators.RSC medicinal chemistry · 2023Article
- Low-molecular-weight anti-HIV-1 agents targeting HIV-1 capsid proteins.RSC advances · 2023Article
- Discovery of novel 1,2,4-triazole phenylalanine derivatives targeting an unexplored region within the interprotomer pocket of the HIV capsid protein.Journal of medical virology · 2022Article
- Design, Synthesis and Structure-Activity Relationships of Phenylalanine-Containing Peptidomimetics as Novel HIV-1 Capsid Binders Based on Ugi Four-Component Reaction.Molecules (Basel, Switzerland) · 2022Article
- Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.European journal of medicinal chemistry · 2022Article
- Rotten to the core: antivirals targeting the HIV-1 capsid core.Retrovirology · 2021Review
- Potency and metabolic stability: a molecular hybrid case in the design of novel PF74-like small molecules targeting HIV-1 capsid protein.RSC medicinal chemistry · 2021Article
- Design, synthesis, and antiviral activity of phenylalanine derivatives as HIV-1 capsid inhibitors.Bioorganic & medicinal chemistry · 2021Article
- Rapid Optimization of the Metabolic Stability of a Human Immunodeficiency Virus Type-1 Capsid Inhibitor Using a Multistep Computational Workflow.Journal of medicinal chemistry · 2021Article
- Design, Synthesis and Characterization of HIV-1 CA-Targeting Small Molecules: Conformational Restriction of PF74.Viruses · 2021Article
- Novel PF74-like small molecules targeting the HIV-1 capsid protein: Balance of potency and metabolic stability.Acta pharmaceutica Sinica. B · 2021Article
- Small-Molecule Anti-HIV-1 Agents Based on HIV-1 Capsid Proteins.Biomolecules · 2021Article
- Structure, Function, and Interactions of the HIV-1 Capsid Protein.Life (Basel, Switzerland) · 2021Review
- Novel HIV-1 capsid-targeting small molecules of the PF74 binding site.European journal of medicinal chemistry · 2020Article
- Chemical profiling of HIV-1 capsid-targeting antiviral PF74.European journal of medicinal chemistry · 2020Article
- Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.Journal of medicinal chemistry · 2020Article
Corrections and comments
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Authors and funding
12 authors at 5 institutions in 3 countries.
Funding
Abstract
The HIV-1 capsid (CA) protein plays essential roles in both early and late stages of HIV-1 replication and is considered an important, clinically unexploited therapeutic target. As such, small drug-like molecules that inhibit this critical HIV-1 protein have become a priority for several groups. Therefore, in this study we explore small molecule targeting of the CA protein, and in particular a very attractive inter-protomer pocket. We report the design, parallel synthesis, and anti-HIV-1 activity evaluation of a series of novel phenylalanine derivatives as HIV-1 CA protein inhibitors synthesized via Cu(I)-catalyzed alkyne-azide 1,3-dipolar cycloaddition (CuAAC) reaction. We demonstrate robust inhibitory activity over a range of potencies against the HIV-1 NL
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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.