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

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F12%3A43871646" target="_blank" >RIV/62157124:16370/12:43871646 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmcl.2012.02.020" target="_blank" >http://dx.doi.org/10.1016/j.bmcl.2012.02.020</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmcl.2012.02.020" target="_blank" >10.1016/j.bmcl.2012.02.020</a>

Result language
angličtina
Original language name
Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries
Original language 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.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Publication year
2012
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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