ArticleJournal of medicinal chemistry2015
Synthesis, Binding and Antiviral Properties of Potent Core-Extended Naphthalene Diimides Targeting the HIV-1 Long Terminal Repeat Promoter G-Quadruplexes.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.
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Who cites it
53 citing papers in PubMed.
- Asymmetric distribution of G-quadruplex forming sequences in genomes of retroviruses.Scientific reports · 2025Article
- Crystal structure, Hirshfeld surface analysis, and DFT and mol-ecular docking studies of 6-cyanona-phthalen-2-yl 4-(benz-yloxy)benzoate.Acta crystallographica. Section E, Crystallographic communications · 2024Article
- Naphthalene Diimide-Tetraazacycloalkane Conjugates Are G-Quadruplex-Based HIV-1 Inhibitors with a Dual Mode of Action.ACS infectious diseases · 2024Article
- G-Quadruplexes in the Regulation of Viral Gene Expressions and Their Impacts on Controlling Infection.Pathogens (Basel, Switzerland) · 2024Review
- Structural and computational studies of HIV-1 RNA.RNA biology · 2024Review
- Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as anti-infectious agents:RSC medicinal chemistry · 2023Article
- G-Quadruplexes in the Viral Genome: Unlocking Targets for Therapeutic Interventions and Antiviral Strategies.Viruses · 2023Review
- DNA topoisomerase 1 represses HIV-1 promoter activity through its interaction with a guanine quadruplex present in the LTR sequence.Retrovirology · 2023Review
- Helquat dyes targeting G-quadruplexes as a new class of anti-HIV-1 inhibitors.Scientific reports · 2023Article
- Targeting G-quadruplexes to achieve antiviral activity.Bioorganic & medicinal chemistry letters · 2023Review
- Deciphering RNA G-quadruplex function during the early steps of HIV-1 infection.Nucleic acids research · 2022Article
- Identification of G-quadruplex DNA sequences in SARS-CoV2.Immunogenetics · 2022Article
- Characterization of G-Quadruplexes in Enterovirus A71 Genome and Their Interaction with G-Quadruplex Ligands.Microbiology spectrum · 2022Article
- Fused in Liposarcoma Protein, a New Player in the Regulation of HIV-1 Transcription, Binds to Known and Newly Identified LTR G-Quadruplexes.ACS infectious diseases · 2022Article
- G-Quadruplex DNA as a Target in Pathogenic Bacteria: Efficacy of an Extended Naphthalene Diimide Ligand and Its Mode of Action.Journal of medicinal chemistry · 2022Article
- Major Achievements in the Design of Quadruplex-Interactive Small Molecules.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Can G-quadruplex become a promising target in HBV therapy?Frontiers in immunology · 2022Review
- Selective Recognition of a Single HIV-1 G-Quadruplex by Ultrafast Small-Molecule Screening.Analytical chemistry · 2021Article
- One-pot synthesis of new alkyl 1-naphthoates bearing quinoline, pyranone and cyclohexenone moietiesRSC advances · 2021Article
- G-Quadruplex Targeting in the Fight against Viruses: An Update.International journal of molecular sciences · 2021Review
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
We have previously reported that stabilization of the G-quadruplex structures in the HIV-1 long terminal repeat (LTR) promoter suppresses viral transcription. Here we sought to develop new G-quadruplex ligands to be exploited as antiviral compounds by enhancing binding toward the viral G-quadruplex structures. We synthesized naphthalene diimide derivatives with a lateral expansion of the aromatic core. The new compounds were able to bind/stabilize the G-quadruplex to a high extent, and some of them displayed clear-cut selectivity toward the viral G-quadruplexes with respect to the human telomeric G-quadruplexes. This feature translated into low nanomolar anti-HIV-1 activity toward two viral strains and encouraging selectivity indexes. The selectivity depended on specific recognition of LTR loop residues; the mechanism of action was ascribed to inhibition of LTR promoter activity in cells. This is the first example of G-quadruplex ligands that show increased selectivity toward the viral G-quadruplexes and display remarkable antiviral activity.
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