期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 8, 页码 3006-3010出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.020
关键词
G-quadruplex; Duplex; DNA; Ligands; NCI Diversity Set; High throughput screen; FRET-based assay; Drug-likeness
资金
- CRUK [C180/A1060, C129/A4489]
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. (C) 2012 Elsevier Ltd. All rights reserved.
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