Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361322 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide