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Macrocyclic G-Quadruplex Ligands

[ Vol. 17 , Issue. 29 ]

Author(s):

M. C. Nielsen and T. Ulven   Pages 3438 - 3448 ( 11 )

Abstract:


G-quadruplex stabilizing compounds have recently received increased interest due to their potential application as anticancer therapeutics. A significant number of structurally diverse G-quadruplex ligands have been developed. Some of the most potent and selective ligands currently known are macrocyclic structures which have been modeled after the natural product telomestatin or from porphyrin-based ligands discovered in the late 1990s. These two structural classes of G-quadruplex ligands are reviewed here with special attention to selectivity and structure-activity relationships, and with focus on the recent developments.

Keywords:

Anticancer therapeutics,DNA,drug discovery,G-quadruplex,macrocycles,porphyrins,ligands,macrocyclic,telomestatin,porphyrin,guanine,nucleic acid,oncogenes,cancer,Hoogsteenbase pairing,topology,telomeric sequences,hybrid,pyrrole,isoindole,Streptomyces anulatus,telomere repeat amplification protocol (TRAP) assay,leukemia,Telomeres,phosphate backbone,hexaoxazoles,tumor xenografts,cytotoxic,HeLa cells,telomerase-negative Saos-2 cells,c-KIT sequence,SPR,FRET Tm,c-MYC,cell line,BCL-2,antitumor,Corroles,p-p stacking,WO 0024747,WO 2004078764

Affiliation:

, Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5320 Odense M, Denmark.



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