ArticleAntimicrobial agents and chemotherapy2003
New anti-human immunodeficiency virus type 1 6-aminoquinolones: mechanism of action.
Article in Antimicrobial agents and chemotherapy, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 58 citations in OpenAlex.
- Anti-HIV-1 Effect of the Fluoroquinolone Enoxacin and Modulation of Pro-Viral hsa-miR-132 Processing in CEM-SS Cells.Non-coding RNA · 2025Article
- Quinolone: a versatile therapeutic compound class.Molecular diversity · 2023Review
- RNA-Binding Macrocyclic Peptides.Frontiers in molecular biosciences · 2022Review
- Advances toward Curing HIV-1 Infection in Tissue Reservoirs.Journal of virology · 2020Review
- Insights into the development of chemical probes for RNA.Nucleic acids research · 2018Article
- Amiloride as a new RNA-binding scaffold with activity against HIV-1 TAR.MedChemComm · 2017Article
- From the traditional Chinese medicine plant Schisandra chinensis new scaffolds effective on HIV-1 reverse transcriptase resistant to non-nucleoside inhibitors.Journal of microbiology (Seoul, Korea) · 2015Article
- Targeting HIV transcription: the quest for a functional cure.Current topics in microbiology and immunology · 2015Review
- Article
- Small molecules targeted to a non-catalytic "RVxF" binding site of protein phosphatase-1 inhibit HIV-1.PloS one · 2012Article
- Early inhibitors of human cytomegalovirus: state-of-art and therapeutic perspectives.Pharmacology & therapeutics · 2011Review
- Discovery of selective bioactive small molecules by targeting an RNA dynamic ensemble.Nature chemical biology · 2011Article
- Herpes simplex virus type 2 infection increases human immunodeficiency virus type 1 entry into human primary macrophages.Virology journal · 2011Article
- The next ten stories on antiviral drug discovery (part E): advents, advances, and adventures.Medicinal research reviews · 2011Review
- A 6-aminoquinolone compound, WC5, with potent and selective anti-human cytomegalovirus activity.Antimicrobial agents and chemotherapy · 2009Article
- Novel in vivo model for the study of human immunodeficiency virus type 1 transcription inhibitors: evaluation of new 6-desfluoroquinolone derivatives.Antimicrobial agents and chemotherapy · 2007Article
- Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.Journal of virology · 2007Article
- Inhibition of human immunodeficiency virus type 1 tat-trans-activation-responsive region interaction by an antiviral quinolone derivative.Antimicrobial agents and chemotherapy · 2004Article
- Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A 6-aminoquinolone derivative, WM5, which bears a methyl substituent at the N-1 position and a 4-(2-pyridyl)-1-piperazine moiety at position 7 of the bicyclic quinolone ring system, was previously shown to exhibit potent activity against replication of human immunodeficiency virus type 1 (HIV-1) in de novo-infected human lymphoblastoid cells (V. Cecchetti et al., J. Med. Chem. 43:3799-3802, 2000). In this report, we further investigated WM5's mechanism of antiviral activity. WM5 inhibited HIV-1 replication in acutely infected cells as well as in chronically infected cells. The 50% inhibitory concentrations were 0.60 +/- 0.06 and 0.85 +/- 0.05 micro M, respectively. When the effects of WM5 on different steps of the virus life cycle were analyzed, the reverse transcriptase activity and the integrase and protease activities were not impaired. By using a transient trans-complementation assay to examine the activity of WM5 on the replicative potential of HIV-1 in a single round of infection, a sustained inhibition of Tat-mediated long terminal repeat (LTR)-driven transcription (>80% of controls) was obtained in the presence of 5 micro M WM5. Interestingly, the aminoquinolone was found to efficiently complex TAR RNA, with a dissociation constant in the nanomolar range (19 +/- 0.6 nM). These data indicate that WM5 is a promising lead compound for the development of a new class of HIV-1 transcription inhibitors characterized by recognition of viral RNA target(s).
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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.