Natural and synthetic G-quadruplex interactive berberine derivatives

Franceschin, Marco; Rossetti, Luigi; D'Ambrosio, A; Schirripa, Stefano; Bianco, Armandodoriano; Ortaggi, Giancarlo; Savino, M.; Schultes, Christoph; Neidle, Stephen

doi:10.1016/j.bmcl.2005.12.001

Cited by 206 publications

(136 citation statements)

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“…9 and 13 substituted berberine derivatives have been reported by Ma et al [27] and Franceschin et al [28], and among the compounds, Compounds 27 and 28 were observed to be the potent telomerase inhibitor by stabilizing G-quadruplex DNA with an IC 50 value of 14 µM.…”

Section: Berberine Derivativesmentioning

confidence: 86%

G-Quadruplex Ligands as Stabilizer Targeting Telomerase Enzyme as Anti Cancer Agents

2017

Asian J Pharm Clin Res

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The human telomere stabilization with G-Quadruplex DNA tends to induce apoptosis. The molecular target of telomere cascade with a rigid molecular may show efficacious to treat cancer. The study of intercalation to human telomeric DNA with proposed ligand can be evaluated by the help of biophysical studies and biological studies. G-Quadruplex is one of the key epigenetic episodes of eukaryotes and prokaryotes, generally found in the telomeric end region, immunoglobulin switch recombination and the lagging strand of the DNA. These chemotherapeutic advances are not enough to maintain a life expectancy of cancer affected patients. A number of G-Quadruplex ligands such as acridine, perylene, and anthraquinones have been synthesized reported and evaluated them for the inhibitor activity. Therefore, translational research can pave the novel prospect to treat cancer in a fundamental way. In that connection, basic research showed G-Quadruplex phenomenon of DNA, which is having a great impact in this chemotherapy.

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Section: Berberine Derivativesmentioning

confidence: 86%

G-Quadruplex Ligands as Stabilizer Targeting Telomerase Enzyme as Anti Cancer Agents

2017

Asian J Pharm Clin Res

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“…Docking has been done by G-Quadruplex Ligand Database (G4LDB). 8,9 This is an online database which was having in built tools and performed by Open Babel 2.3.0 to predict the binding affinity with the targets. The targets (1LIH, 1NZM, 3CE5, 3SC8 and 2HRI) for the docking are selected based upon the literature survey and the selected compounds are docked.…”

Section: Results and Conclusionmentioning

confidence: 99%

Application of 3D QSAR and Docking Studies in Optimization of Perylene di imides as Anti Cancer Agent

Hemalatha¹,

Muthkumar²

2018

IJPER

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Introduction:Telomerase is an enzyme which binds to telomeres and increases its length which leads to extension of lifespan of cells. These enzymes are expressed at detectable levels in cancer cells which makes an attractive target for cancer therapy. The G Quadruplex ligands which bind to telomerase with respect to duplex genomic DNA is of special importance. The Perylene di imides are selected, designed and QSAR study has been done, finally from the QSAR results' docking has been done by G4LDB database. To compare and to narrow down the Docking results from G4LDB database, we have chosen AutoDock tool by selecting a target Telomerase protein (PDB ID: 4B18) to analyse the binding affinity of the protein with respect to the Perylene diimides. The best scored compounds will be efficient for designing new molecules as well as for the anti-cancer therapy. G4LDB and AutoDock), 3 compounds (11, 20 and 48) showed good biological activity possessing a strong correlation coefficient, endorses that Perylene derivatives are having strong affinity with the targets. Docking has been done from the results of QSAR study, targeting Telomerase protein to study the binding affinity with the target. Conclusions: From the results, the best compounds will be efficient to inhibit telomerase enzyme and these compounds can be used to design new molecules which will be effective for anticancer therapy.

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“…Q2), albeit more weakly than the parent berberine, but in common with berberine, did not induce folding of an intramolecular qDNA. 6 These experiments and others 19 highlight the utility of ESI-MS for screening ligand-binding to qDNA. The 13-substituted berberine derivatives (2-4, 5 and 7) have a substantial binding preference for the tetrameric intermolecular qDNA, Q4.…”

mentioning

confidence: 89%

“…1) and its 13-piperidino derivative show moderate and approximately equal abilities to stabilise an intramolecular qDNA as judged by thermal melting experiments. 6 Coralyne, a synthetic derivative of berberine with a fully aromatic core, shows a much greater stabilising effect against melting. 6 Recently we showed using electrospray ionisation mass spectrometry (ESI-MS) that a berberine derivative substituted at its 13-position with a 5-nitro-2-phenylindolylmethyl group (2) had modest binding affinity for a tetrameric qDNA, and significant selectivity over duplex DNA.…”

mentioning

confidence: 99%

“…6 Coralyne, a synthetic derivative of berberine with a fully aromatic core, shows a much greater stabilising effect against melting. 6 Recently we showed using electrospray ionisation mass spectrometry (ESI-MS) that a berberine derivative substituted at its 13-position with a 5-nitro-2-phenylindolylmethyl group (2) had modest binding affinity for a tetrameric qDNA, and significant selectivity over duplex DNA. 7 Compound 2 and its meta and para isomers, 3 and 4 ( Fig.…”

mentioning

confidence: 99%

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A mass spectrometric investigation of novel quadruplex DNA-selective berberine derivatives

et al. 2010

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Natural and synthetic G-quadruplex interactive berberine derivatives

Cited by 206 publications

References 23 publications

G-Quadruplex Ligands as Stabilizer Targeting Telomerase Enzyme as Anti Cancer Agents

G-Quadruplex Ligands as Stabilizer Targeting Telomerase Enzyme as Anti Cancer Agents

Application of 3D QSAR and Docking Studies in Optimization of Perylene di imides as Anti Cancer Agent

A mass spectrometric investigation of novel quadruplex DNA-selective berberine derivatives

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