title: Synthesis of Macrocyclic Hexaoxazole (6OTD) Dimers, Containing Guanidine and Amine Functionalized Side Chains, and an Evaluation of Their Telomeric G4 Stabilizing Properties.
abstract: Structure-activity relationship studies were carried out on macrocyclic hexaoxazole (6OTD) dimers, whose core structure stabilizes telomeric G-quadruplexes (G4). Two new 6OTD dimers having side chain amine and guanidine functional groups were synthesized and evaluated for their stabilizing ability against a telomeric G4 DNA sequence. The results show that the 6OTD dimers interact with the DNA to form 1:1 complexes and stabilize the antiparallel G4 structure of DNA in the presence of potassium cation. The guanidine functionalized dimer displays a potent stabilizing ability of the G4 structure, as determined by using a FRET melting assay (DeltaT(m) = 14 degrees C).
authors.affiliation: Department of Biotechnology and Life Science Faculty of Technology, Tokyo University of Agriculture and Technology (TUAT), Koganei, Tokyo 184-8588, Japan.
authors.forename: Keisuke
authors.initials: K
authors.lastname: Iida
authors.forename: Masayuki
authors.initials: M
authors.lastname: Tera
authors.forename: Takatsugu
authors.initials: T
authors.lastname: Hirokawa
authors.forename: Kazuo
authors.initials: K
authors.lastname: Shin-Ya
authors.forename: Kazuo
authors.initials: K
authors.lastname: Nagasawa