Synthesis and evaluation of 2,9-disubstituted-1,10-phenanthroline derivatives as G-quadruplex binders
Identifikátory výsledku
Kód výsledku v 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>
Výsledek na webu
<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>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Synthesis and evaluation of 2,9-disubstituted-1,10-phenanthroline derivatives as G-quadruplex binders
Popis výsledku v původním jazyce
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).
Název v anglickém jazyce
Synthesis and evaluation of 2,9-disubstituted-1,10-phenanthroline derivatives as G-quadruplex binders
Popis výsledku anglicky
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).
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
10608 - Biochemistry and molecular biology
Návaznosti výsledku
Projekt
<a href="/cs/project/EF15_003%2F0000477" target="_blank" >EF15_003/0000477: Strukturní gymnastika nukleových kyselin: od molekulárních principů přes biologické funkce k terapeutickým cílům.</a><br>
Návaznosti
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2022
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Bioorganic & Medicinal Chemistry
ISSN
0968-0896
e-ISSN
1464-3391
Svazek periodika
73
Číslo periodika v rámci svazku
NOV 1 2022
Stát vydavatele periodika
GB - Spojené království Velké Británie a Severního Irska
Počet stran výsledku
10
Strana od-do
116971
Kód UT WoS článku
000868425800001
EID výsledku v databázi Scopus
2-s2.0-85139346147