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Communication | Special issue | Vol 84, No. 1, 2012, pp. 401 - 411
Published online: 13th September, 2011
DOI: 10.3987/COM-11-S(P)88
Design and Synthesis of G-Quadruplex Ligands Bearing Macrocyclic Hexaoxazoles with Four-Way Side Chains

Keisuke Iida, Satoki Majima, Terumi Ohtake, Masayuki Tera, Kazuo Shin-ya, and Kazuo Nagasawa*

*Division of Biotechnology and Life Science, Institute of Symbiotic Science and Technology, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei, Tokyo 184-8588, Japan

Abstract

Macrocyclic hexaoxazole compounds bearing four-way side chains L2H2-(4M)6OTD derivatives 3 and 4 were synthesized as new G-quadruplex ligands. Stabilization of G-quadruplex forming oligonucleotides in human telomeres, c-kit, bcl-2, and c-myc with those compounds was evaluated by the FRET (fluorescence resonance energy transfer) assay. These compounds showed less stabilizing ability compared to the ligand possessing two-way side chain of L2H2-(4M)6OTD (2d).

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