ArticleEuropean journal of medicinal chemistry2022
Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.
Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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The trial behind it
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Who cites it
10 citing papers in PubMed, 24 citations in OpenAlex.
- New Advances in Anti-HIV-1 Strategies Targeting the Assembly and Stability of Capsid Protein.International journal of molecular sciences · 2025Review
- Synthesis, Cytotoxicity and Antiproliferative Effect of New Pyrrole Hydrazones.Molecules (Basel, Switzerland) · 2024Article
- Synthesis, crystal structure, and antiviral evaluation of new imidazopyridine-schiff base derivatives:RSC advances · 2024Article
- Design and Synthesis of New GS-6207 Subtypes for Targeting HIV-1 Capsid Protein.International journal of molecular sciences · 2024Article
- Facile synthesis andFuture medicinal chemistry · 2024Article
- Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.Journal of medicinal chemistry · 2023Article
- Discovery and Mechanistic Investigation of Piperazinone Phenylalanine Derivatives with Terminal Indole or Benzene Ring as Novel HIV-1 Capsid Modulators.Molecules (Basel, Switzerland) · 2022Article
- 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 Mechanistic Study of 2-Pyridone-Bearing Phenylalanine Derivatives as Novel HIV Capsid Modulators.Molecules (Basel, Switzerland) · 2022Article
- Metabolite Identification of HIV-1 Capsid Modulators PF74 and 11L in Human Liver Microsomes.Metabolites · 2022Article
Corrections and comments
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Authors and funding
19 authors at 4 institutions in 4 countries.
Funding
Abstract
Further clinical development of PF74, a lead compound targeting HIV-1 capsid, is impeded by low antiviral activity and inferior metabolic stability. By modifying the benzene (region I) and indole of PF74, we identified two potent compounds (7m and 7u) with significantly improved metabolic stability. Compared to PF74, 7u displayed greater metabolic stability in human liver microsomes (HLMs) with half-life (t
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Registered trials
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