ArticleEuropean journal of medicinal chemistry2022
Novel nucleocapsid protein-targeting phenanthridine inhibitors of SARS-CoV-2.
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 14 papers.
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Who cites it
14 citing papers in PubMed, 34 citations in OpenAlex.
- Nanoplasmonic optical fiber sensing of SARS-CoV-2 nucleocapsid protein using an aptamer-DNA tetrahedron interface.Journal of nanobiotechnology · 2026Article
- Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- New Advances in Small Molecules Targeted at Viral Capsid-Genome Binding.International journal of molecular sciences · 2025Review
- Bridging chemical space and biological efficacy: advances and challenges in applying generative models in structural modification of natural products.Natural products and bioprospecting · 2025Review
- Ciclopirox inhibits SARS-CoV-2 replication by promoting the degradation of the nucleocapsid protein.Acta pharmaceutica Sinica. B · 2024Article
- Discovery of novel phenanthridone derivatives with anti-streptococcal activity.Archives of microbiology · 2023Article
- Article
- Synthesis of 5,6-Dihydrophenanthridines via Palladium-Catalyzed Intramolecular Dehydrogenative Coupling of Two Aryl C-H Bonds.Molecules (Basel, Switzerland) · 2023Article
- Lessons Learnt from COVID-19: Computational Strategies for Facing Present and Future Pandemics.International journal of molecular sciences · 2023Review
- Recent advances in applying G-quadruplex for SARS-CoV-2 targeting and diagnosis: A review.International journal of biological macromolecules · 2022Review
- Recent Advances of Representative Optical Biosensors for Rapid and Sensitive Diagnostics of SARS-CoV-2.Biosensors · 2022Review
- Computational exploration of the dual role of the phytochemical fortunellin: Antiviral activities against SARS-CoV-2 and immunomodulatory abilities against the host.Computers in biology and medicine · 2022Article
- Borneol Ester Derivatives as Entry Inhibitors of a Wide Spectrum of SARS-CoV-2 Viruses.Viruses · 2022Article
- Identification and characterization of alternative sites and molecular probes for SARS-CoV-2 target proteins.Frontiers in chemistry · 2022Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is unprecedented in human history. As a major structural protein, nucleocapsid protein (NPro) is critical to the replication of SARS-CoV-2. In this work, 17 NPro-targeting phenanthridine derivatives were rationally designed and synthesized, based on the crystal structure of NPro. Most of these compounds can interact with SARS-CoV-2 NPro tightly and inhibit the replication of SARS-CoV-2 in vitro. Compounds 12 and 16 exhibited the most potent anti-viral activities with 50% effective concentration values of 3.69 and 2.18 μM, respectively. Furthermore, site-directed mutagenesis of NPro and Surface Plasmon Resonance (SPR) assays revealed that 12 and 16 target N-terminal domain (NTD) of NPro by binding to Tyr109. This work found two potent anti-SARS-CoV-2 bioactive compounds and also indicated that SARS-CoV-2 NPro-NTD can be a target for new anti-virus agents.
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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.