ArticleFrontiers in chemistry2014
Bis-indole derivatives with antitumor activity turn out to be specific ligands of human telomeric G-quadruplex.
Article in Frontiers in chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Effects of hydrazone-based G-quadruplex ligands onNAR cancer · 2025Article
- Pursuing Polypharmacology: Benzothiopyranoindoles as G-Quadruplex Stabilizers and Topoisomerase I Inhibitors for Effective Anticancer Strategies.ACS medicinal chemistry letters · 2024Article
- Screening of the Pandemic Response Box identifies anti-microsporidia compounds.PLoS neglected tropical diseases · 2023Article
- Targeting of Telomeric Repeat-Containing RNA G-Quadruplexes: From Screening to Biophysical and Biological Characterization of a New Hit Compound.International journal of molecular sciences · 2021Article
- Synthesis and in Vitro Evaluation of Novel 5-Nitroindole Derivatives as c-Myc G-Quadruplex Binders with Anticancer Activity.ChemMedChem · 2021Article
- Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells.Journal of medicinal chemistry · 2020Article
- Spiro-Indole-Coumarin Hybrids: Synthesis, ADME, DFT, NBO Studies and In Silico Screening through Molecular Docking on DNA G-Quadruplex.ChemistrySelect · 2020Article
- Insights into telomeric G-quadruplex DNA recognition by HMGB1 protein.Nucleic acids research · 2019Article
- Common G-Quadruplex Binding Agents Found to Interact With i-Motif-Forming DNA: Unexpected Multi-Target-Directed Compounds.Frontiers in chemistry · 2018Article
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Authors and funding
11 authors.
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Abstract
Bis-indolinone derivatives having either 2,6-disubstituted pyridine core (1a and 1b) or 1,10-disubstituted phenanthroline core (2a and 2b), already known to have antitumor activity, have been tested as potential G-quadruplex binders. Compounds 2a and 2b are able to selectively stabilize G-quadruplex over duplex DNA, and also to discriminate among different G-quadruplex structures, having a particular affinity for the parallel form of the human telomeric G-quadruplex. Both compounds are also able to induce telomeric DNA damage that may explain the activity of these compounds.
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