ArticleBioorganic & medicinal chemistry letters2010
Design, synthesis, and evaluation of indole compounds as novel inhibitors targeting Gp41.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Small-Molecule HIV Entry Inhibitors Targeting gp120 and gp41.Advances in experimental medicine and biology · 2022Review
- Evaluation of ligand-based NMR screening methods to characterize small molecule binding to HIV-1 glycoprotein-41.Organic & biomolecular chemistry · 2017Article
- Development of Small-molecule HIV Entry Inhibitors Specifically Targeting gp120 or gp41.Current topics in medicinal chemistry · 2016Review
- A review on recent developments of indole-containing antiviral agents.European journal of medicinal chemistry · 2015Review
- Structure-activity relationship studies of indole-based compounds as small molecule HIV-1 fusion inhibitors targeting glycoprotein 41.Journal of medicinal chemistry · 2014Article
- Identification of fragments targeting an alternative pocket on HIV-1 gp41 by NMR screening and similarity searching.Bioorganic & medicinal chemistry letters · 2013Article
- Review
- Computer-Aided Approaches for Targeting HIVgp41.Biology · 2012Article
- Biochemistry and biophysics of HIV-1 gp41 - membrane interactions and implications for HIV-1 envelope protein mediated viral-cell fusion and fusion inhibitor design.Current topics in medicinal chemistry · 2011Review
- Targeting HIV-1 gp41-induced fusion and pathogenesis for anti-viral therapy.Current topics in medicinal chemistry · 2011Review
- Amphipathic properties of HIV-1 gp41 fusion inhibitors.Current topics in medicinal chemistry · 2011Review
- Development of indole compounds as small molecule fusion inhibitors targeting HIV-1 glycoprotein-41.Journal of medicinal chemistry · 2011Article
- Paramagnetic relaxation assisted docking of a small indole compound in the HIV-1 gp41 hydrophobic pocket.ACS chemical biology · 2011Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant of compound 7 was 2.1microM, and the IC(50) for cell-cell fusion inhibition was 1.1microM. Assay data indicated that 7 is a promising lead compound for optimization into an effective low molecular weight fusion inhibitor.
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Registered trials
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