About: Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries

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About: Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Thirteen compounds with diverse chemical structures have been identified as selective telomeric G-quadruplex-binding ligands through screening the NCI Diversity Set II, the NCI Natural Products Set II and the NCI Mechanistic Diversity Set libraries containing a total of 2307 members against a human telomeric G-quadruplex using a FRET-based DNA melting assay. These compounds show significant selectivity towards a telomeric G-quadruplex compared to duplex DNA, fall within a molecular weight range of 327-533, and are generally consistent with the Lipinski Rule of Five for drug-likeness. Thus they provide new chemical scaffolds for the development of novel classes of G-quadruplex-targeting agents. Thirteen compounds with diverse chemical structures have been identified as selective telomeric G-quadruplex-binding ligands through screening the NCI Diversity Set II, the NCI Natural Products Set II and the NCI Mechanistic Diversity Set libraries containing a total of 2307 members against a human telomeric G-quadruplex using a FRET-based DNA melting assay. These compounds show significant selectivity towards a telomeric G-quadruplex compared to duplex DNA, fall within a molecular weight range of 327-533, and are generally consistent with the Lipinski Rule of Five for drug-likeness. Thus they provide new chemical scaffolds for the development of novel classes of G-quadruplex-targeting agents. (en)
Title	Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries (en)
skos:prefLabel	Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries (en)
skos:notation	RIV/62157124:16370/12:43871646!RIV13-MSM-16370___
http://linked.open...avai/riv/aktivita	V
http://linked.open...avai/riv/aktivity	V
http://linked.open...iv/cisloPeriodika	8
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Tížková, Karolina
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Veterinární a farmaceutická univerzita Brno / Farmaceutická fakulta
http://linked.open...dnocenehoVysledku	140315
http://linked.open...ai/riv/idVysledku	RIV/62157124:16370/12:43871646
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Drug-likeness; FRET-based assay; High throughput screen; NCI Diversity Set; Ligands; DNA; Duplex (en)
http://linked.open.../riv/klicoveSlovo	DNA Drug-likeness Duplex FRET-based assay High throughput screen Ligands NCI Diversity Set
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[15AF76EDA56B]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	1 (xsd:int)
http://linked.open...cetTvurcuVysledku	5 (xsd:int)
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	22
http://linked.open...iv/tvurceVysledku	Khondaker, Rahman Neidle, Stephen Reszka, Anthony Thurston, David Tížková, Karolina
http://linked.open...ain/vavai/riv/wos	000302768200077
issn	0960-894X
number of pages	5 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2012.02.020
http://localhost/t...ganizacniJednotka	16370

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