scholarly journals Anticancer Activity and Cellular Repression of c-MYC by the G-Quadruplex-Stabilizing 11-Piperazinylquindoline Is Not Dependent on Direct Targeting of the G-Quadruplex in the c-MYC Promoter

2012 ◽  
Vol 55 (13) ◽  
pp. 6076-6086 ◽  
Author(s):  
Peda V. L. Boddupally ◽  
Seongmin Hahn ◽  
Cristina Beman ◽  
Biswanath De ◽  
Tracy A. Brooks ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
G Quadruplex ◽  
Direct Targeting

scholarly journals Naphthalenediimide-Linked Bisbenzimidazole Derivatives as Telomeric G-Quadruplex-Stabilizing Ligands with Improved Anticancer Activity

ACS Omega ◽  
2017 ◽  
Vol 2 (3) ◽  
pp. 966-980 ◽  
Author(s):  
Souvik Sur ◽  
Vinod Tiwari ◽  
Devapriya Sinha ◽  
Mohammad Zahid Kamran ◽  
Kshatresh Dutta Dubey ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
G Quadruplex ◽  
Stabilizing Ligands

scholarly journals On the interaction of an anticancer trisubstituted naphthalene diimide with G-quadruplexes of different topologies: a structural insight

2020 ◽  
Vol 48 (21) ◽  
pp. 12380-12393
Author(s):  
Chiara Platella ◽  
Marko Trajkovski ◽  
Filippo Doria ◽  
Mauro Freccero ◽  
Janez Plavec ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Dissociation Constants ◽  
Therapeutic Potential ◽  
In Vivo Studies ◽  
Binding Modes ◽  
Hybrid Topology ◽  
Naphthalene Diimide ◽  
G Quadruplex ◽  
Naphthalene Diimides

Abstract Naphthalene diimides showed significant anticancer activity in animal models, with therapeutic potential related to their ability to strongly interact with G-quadruplexes. Recently, a trifunctionalized naphthalene diimide, named NDI-5, was identified as the best analogue of a mini-library of novel naphthalene diimides for its high G-quadruplex binding affinity along with marked, selective anticancer activity, emerging as promising candidate drug for in vivo studies. Here we used NMR, dynamic light scattering, circular dichroism and fluorescence analyses to investigate the interactions of NDI-5 with G-quadruplexes featuring either parallel or hybrid topology. Interplay of different binding modes of NDI-5 to G-quadruplexes was observed for both parallel and hybrid topologies, with end-stacking always operative as the predominant binding event. While NDI-5 primarily targets the 5′-end quartet of the hybrid G-quadruplex model (m-tel24), the binding to a parallel G-quadruplex model (M2) occurs seemingly simultaneously at the 5′- and 3′-end quartets. With parallel G-quadruplex M2, NDI-5 formed stable complexes with 1:3 DNA:ligand binding stoichiometry. Conversely, when interacting with hybrid G-quadruplex m-tel24, NDI-5 showed multiple binding poses on a single G-quadruplex unit and/or formed different complexes comprising two or more G-quadruplex units. NDI-5 produced stabilizing effects on both G-quadruplexes, forming complexes with dissociation constants in the nM range.

Anticancer Activity for Targeting Telomeric G-Quadruplex and Antiangiogenesis of a Novel Ru(II)–Se Complex

2014 ◽  
Vol 157 (2) ◽  
pp. 175-182 ◽  
Author(s):  
Lijun Wang ◽  
Chuping Zheng ◽  
Yanyu Liu ◽  
Fangling Le ◽  
Fang Yang ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
G Quadruplex

Anticancer activity of novel ruthenium complex with 1,10-phenanthrolineselenazole as potent telomeric G-quadruplex inhibitor

2012 ◽  
Vol 20 ◽  
pp. 142-146 ◽  
Author(s):  
Qian Li ◽  
Dongdong Sun ◽  
Yanhui Zhou ◽  
Du Liu ◽  
Qianling Zhang ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Ruthenium Complex ◽  
G Quadruplex

Stabilization for loop isomers of c-myc G-quadruplex DNA and anticancer activity by ruthenium complexes

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1724-1728 ◽  
Author(s):  
Ying Liu ◽  
Yanan Liu ◽  
Licong Yang ◽  
Chengwen Cao ◽  
Yanhui Zhou ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Ruthenium Complexes ◽  
Quadruplex Dna ◽  
G Quadruplex

Telomere DNA Binding, Cleavage and Anticancer Activity of [Cu(phendione)(Hpyramol)Cl]

2019 ◽  
Vol 13 (2) ◽  
pp. 171-182
Author(s):  
Palanisamy Uma Maheswari ◽  
Renuga Duraisamy ◽  
Murugesan Kanagavel ◽  
Kalimuthusamy Natarajaseenivasan ◽  
Kadhar Mohamed Meera Sheriffa Begum ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Dna Cleavage ◽  
Phenoxyl Radical ◽  
Anticancer Activities ◽  
Redox Active ◽  
G Quadruplex ◽  
Ic50 Values ◽  
Controlled Potential ◽  
Human Telomere

Background:The ligand Hpyramol is a redox active, which on coordination with Cu(II) cleaves DNA without any added reductant. Another ligand phendione is known for its wide application towards anticancer activities. We combined the ligands with CuCl2 to have an intercalation moiety and a redox active ligand in participation towards telomere DNA cleavage and anticancer activity.Objective:In this study, our aim is to interact it with Human telomere DNA and to see their effects on cancer cells.Methods:The complex [Cu(L)(L’)Cl] has interacted with the human telomere DNA sequence (TTAGGG), HTelo20. The HTelo20 was stabilized under both parallel and antiparallel G-quadruplex conformations and the complex [Cu(L)(L’)Cl] has interacted followed by circular dichroism spectroscopy and gel electrophoresis.Results:The parallel G-quadruplex and randomly coiled conformations of HTelo20 were easily cleaved than the anti-parallel G-quadruplex conformation. The nature of DNA cleavage was found to be oxidative rather hydrolytic. The formation of phenoxyl radical species under electrochemical and controlled potential electrolysis conditions by the complex [Cu(L)(L’)Cl] proves the possibility of oxidative nature of DNA cleavage. The comet assay also proves the DNA cleavage induced by the complex [Cu(L)(L’)Cl] inside the nucleus of HeLa cancer cells.Conclusion:The complex [Cu(L)(L’)Cl] was tested for anticancer activity, induced by ROS and DNA cleavage. The IC50 values resulted in nanomolar concentrations with selected cancer cell lines. Relatively the Cu complex shows less toxicity with the normal cell line L132.

Bio-Inspired Dual-Selective BCL-2/c-MYC G-Quadruplex Binders: Design, Synthesis, and Anticancer Activity of Drug-like Imidazo[2,1-i]purine Derivatives

2019 ◽  
Vol 63 (5) ◽  
pp. 2035-2050 ◽  
Author(s):  
Sveva Pelliccia ◽  
Jussara Amato ◽  
Domenica Capasso ◽  
Sonia Di Gaetano ◽  
Alberto Massarotti ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Purine Derivatives ◽  
Design Synthesis ◽  
G Quadruplex

scholarly journals Naphthalene Diimides as Multimodal G-Quadruplex-Selective Ligands

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 426 ◽  
Author(s):  
Valentina Pirota ◽  
Matteo Nadai ◽  
Filippo Doria ◽  
Sara Richter
Keyword(s):  
Anticancer Activity ◽  
Biomedical Applications ◽  
Antimicrobial Agents ◽  
Binding Modes ◽  
High Affinity ◽  
Naphthalene Diimide ◽  
G Quadruplex ◽  
Selective Ligands ◽  
Genomic Regions ◽  
Naphthalene Diimides

G-quadruplexes are four-stranded nucleic acids structures that can form in guanine-rich sequences. Following the observation that G-quadruplexes are particularly abundant in genomic regions related to cancer, such as telomeres and oncogenes promoters, several G-quadruplex-binding molecules have been developed for therapeutic purposes. Among them, naphthalene diimide derivatives have reported versatility, consistent selectivity and high affinity toward the G-quadruplex structures. In this review, we present the chemical features, synthesis and peculiar optoelectronic properties (absorption, emission, redox) that make naphtalene diimides so versatile for biomedical applications. We present the latest developments on naphthalene diimides as G-quadruplex ligands, focusing on their ability to bind G-quadruplexes at telomeres and oncogene promoters with consequent anticancer activity. Their different binding modes (reversible versus irreversible/covalent) towards G-quadruplexes and their additional use as antimicrobial agents are also presented and discussed.

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