Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers.
A series of diarylurea ligands were designed to interact selectively with G-quadruplexes and were synthesised using copper(I) catalysed 'click' chemistry to incorporate the 1,4-substituted 1,2,3-triazole ring into the core of the ligands; the optimal ligands demonstrate a high degree of selective telomeric G-quadruplex stabilisation and are not cytotoxic in several cancer cell lines.
Drewe
William C
WC
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London, UK.
Neidle
Stephen
S
D000818:Animals; D001665:Binding Sites; D002384:Catalysis; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003300:Copper / Q000737:chemistry; D004247:DNA / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D014230:Triazoles / Q000737:chemistry*; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry*
D008024:Ligands; D014230:Triazoles; D003300:Copper; D014508:Urea; D004247:DNA