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Paper | Special issue | Vol 82, No. 2, 2011, pp. 1345 - 1357
Published online: 13th August, 2010
DOI: 10.3987/COM-10-S(E)85
Design and Synthesis of Telomestatin Derivatives Containing Methyl Oxazole and Their G-Quadruplex Stabilizing Activities

Satoki Majima, Masayuki Tera, Keisuke Iida, 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

Telomestatin derivatives of L2A2-6M(2)OTD (3b) and L2A2-6M(4)OTD (3c), which have a macrocyclic hexaoxazole skeleton (6OTD) containing bis- and tetra-methyl oxazoles, were synthesized as a novel G-quadruplex ligand. This new class of “methyl oxazole containing” ligands was revealed to stabilize various G-quadruplex forming oligonucleotides more potently than “no methyl oxazole containing” L2A2-6OTD (3a).

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