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

Rahman, K.M., Tizkova, K., Reszka, A.P., Neidle, S. and Thurston, D.E. (2012) Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries. Bioorganic and Medicinal Chemistry Letters, 22 (8). pp. 3006-3010. 10.1016/j.bmcl.2012.02.020.

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DOI: 10.1016/j.bmcl.2012.02.020

Abstract

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.

Item Type:Article
Uncontrolled Keywords:G-quadruplex; Duplex; DNA; Ligands; NCI Diversity Set; High throughput screen; FRET-based assay; Drug-likeness
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:3156
Journal or Publication Title:Bioorganic and Medicinal Chemistry Letters
Deposited By:Library Staff
Deposited On:03 May 2012 16:30
Last Modified:03 May 2012 16:30

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