ArticleBioorganic & medicinal chemistry2011
Virtual screening based identification of novel small-molecule inhibitors targeted to the HIV-1 capsid.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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.
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.
Who cites it
26 citing papers in PubMed, 64 citations in OpenAlex.
- Docking, Synthesis and Evaluation of 4-hydroxy-1-phenyl-2(1H)-quinolone Derivatives as Anticancer Agents.Current drug discovery technologies · 2024Article
- Quinolone: a versatile therapeutic compound class.Molecular diversity · 2023Review
- Antiviral compounds modulate elasticity, strength and material fatigue of a virus capsid framework.Biophysical journal · 2022Article
- Review
- In Silico Drug Discovery for Treatment of Virus Diseases.Advances in experimental medicine and biology · 2022Article
- 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.European journal of medicinal chemistry · 2020Article
- HIV Capsid Inhibitors Beyond PF74.Diseases (Basel, Switzerland) · 2019Review
- A HTRF based competitive binding assay for screening specific inhibitors of HIV-1 capsid assembly targeting the C-Terminal domain of capsid.Antiviral research · 2019Article
- Discovery and Development of Anti-HIV Therapeutic Agents: Progress Towards Improved HIV Medication.Current topics in medicinal chemistry · 2019Review
- GS-CA Compounds: First-In-Class HIV-1 Capsid Inhibitors Covering Multiple Grounds.Frontiers in microbiology · 2019Article
- Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library.European journal of medicinal chemistry · 2018Article
- Gold-catalyzed post-Ugi alkyne hydroarylation for the synthesis of 2-quinolones.Beilstein journal of organic chemistry · 2018Article
- Comparison of Biochemical Properties of HIV-1 and HIV-2 Capsid Proteins.Frontiers in microbiology · 2017Article
- HIV-1 capsid is involved in post-nuclear entry steps.Retrovirology · 2016Article
- Identification of a small molecule HIV-1 inhibitor that targets the capsid hexamer.Bioorganic & medicinal chemistry letters · 2016Article
- Article
- HIV-1 Capsid Inhibitors as Antiretroviral Agents.Current HIV research · 2016Review
- STRUCTURAL VIROLOGY. X-ray crystal structures of native HIV-1 capsid protein reveal conformational variability.Science (New York, N.Y.) · 2015Article
- Structure-activity relationships of a novel capsid targeted inhibitor of HIV-1 replication.Journal of chemical information and modeling · 2014Article
- Dual-acting stapled peptides target both HIV-1 entry and assembly.Retrovirology · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The hydrophobic cavity of the C-terminal domain (CTD) of HIV-1 capsid has been recently validated as potential target for antiviral drugs by peptide-based inhibitors; however, there is no report yet of any small molecule compounds that target this hydrophobic cavity. In order to fill this gap and discover new classes of ant-HIV-1 inhibitors, we undertook a docking-based virtual screening and subsequent analog search, and medicinal chemistry approaches to identify small molecule inhibitors against this target. This article reports for the first time, to the best of our knowledge, identification of diverse classes of inhibitors that efficiently inhibited the formation of mature-like viral particles verified under electron microscope (EM) and showed potential as anti-HIV-1 agents in a viral infectivity assay against a wide range of laboratory-adapted as well as primary isolates in MT-2 cells and PBMC. In addition, the virions produced after the HIV-1 infected cells were treated with two of the most active compounds showed drastically reduced infectivity confirming the potential of these compounds as anti-HIV-1 agents. We have derived a comprehensive SAR from the antiviral data. The SAR analyses will be useful in further optimizing the leads to potential anti-HIV-1 agents.
Indexed as
Identifiers
What OpenQuestion holds
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.