Synthesis and evaluation of 2,9-disubstituted-1,10-phenanthroline derivatives as G-quadruplex binders

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F22%3A00563244" target="_blank" >RIV/68081707:_____/22:00563244 - isvavai.cz</a>
Result on the web
<a href="https://reader.elsevier.com/reader/sd/pii/S0968089622003649?token=A4EAFEEB1A2D211C650C572D440F273643EE887CF8238E8B72F14E24D6A6E20A00CA5CE417490443521225405C2455A0&originRegion=eu-west-1&originCreation=20221108091428" target="_blank" >https://reader.elsevier.com/reader/sd/pii/S0968089622003649?token=A4EAFEEB1A2D211C650C572D440F273643EE887CF8238E8B72F14E24D6A6E20A00CA5CE417490443521225405C2455A0&originRegion=eu-west-1&originCreation=20221108091428</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2022.116971" target="_blank" >10.1016/j.bmc.2022.116971</a>

Result language
angličtina
Original language name
Synthesis and evaluation of 2,9-disubstituted-1,10-phenanthroline derivatives as G-quadruplex binders
Original language description
G-quadruplex (G4) structures are non-canonical DNA/RNA secondary structures able to form within guanine rich nucleic acids sequences. They are present in several regions of the human genome including gene promoters, untranslated sequences, and telomeres. Due to their biological relevance G4 structures are considered important drug targets, in particular for anticancer therapies, leading to the development of G4 stabilizing small molecules. Telomeric regions have received special attention in this field since they can fold into several distinct intramolecular G-quadruplexes topologies. Herein, we report the synthesis of 2,9-disubstituted-1,10-phenanthroline derivatives and their ability to stabilize different intramolecular telomeric G4 sequences.We evaluated ligand-induced stabilization, selectivity and specificity of ligands using Fo spacing diaeresis rster Resonance Energy Transfer (FRET) melting experiments and circular dichroism (CD). In addition, we assessed the cytotoxicity of ligands against two cancer cell lines (A549 and H1299) and one healthy cell line (NHDF).
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology

Project
<a href="/en/project/EF15_003%2F0000477" target="_blank" >EF15_003/0000477: Structural gymnastics of nucleic acids: from molecular principles through biological functions to therapeutic targets.</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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