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
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