2021
DOI: 10.3390/pharmaceutics13101611
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Identification of Effective Anticancer G-Quadruplex-Targeting Chemotypes through the Exploration of a High Diversity Library of Natural Compounds

Abstract: In the quest for selective G-quadruplex (G4)-targeting chemotypes, natural compounds have been thus far poorly explored, though representing appealing candidates due to the high structural diversity of their scaffolds. In this regard, a unique high diversity in-house library composed of ca. one thousand individual natural products was investigated. The combination of molecular docking-based virtual screening and the G4-CPG experimental screening assay proved to be useful to quickly and effectively identify—out… Show more

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Cited by 15 publications
(25 citation statements)
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References 82 publications
(98 reference statements)
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“…Finally, biological assays indicated Chelidonine and Rotenone as the most active anticancer compounds, with IC 50 values of 0.64 and 0.15 μ m , respectively, on BJ‐EHLT cancer cells, and also showing a good selectivity over normal BJ‐hTERT cells. [32] …”
Section: Optimization Of the G4‐binding Assays: G4‐cpg Assay And Its ...mentioning
confidence: 99%
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“…Finally, biological assays indicated Chelidonine and Rotenone as the most active anticancer compounds, with IC 50 values of 0.64 and 0.15 μ m , respectively, on BJ‐EHLT cancer cells, and also showing a good selectivity over normal BJ‐hTERT cells. [32] …”
Section: Optimization Of the G4‐binding Assays: G4‐cpg Assay And Its ...mentioning
confidence: 99%
“…[ 25 , 26 ] Specific G4 binding modes include stacking on the outer G‐quartets and/or on nucleobases in loops or in the flanking segments, and/or binding at the grooves or loops mediated by hydrogen bonds or electrostatic interactions. [ 28 , 29 , 30 , 31 , 32 ]…”
Section: Introductionmentioning
confidence: 99%
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