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.
Full text not available from this repository.
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.
|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|
|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|
Item downloaded times since 03 May 2012 16:30.
Repository Staff Only: Item control page
School of Pharmacy Staff Only: Edit a copy to replace this item