Lysinyl macrocyclic hexaoxazoles: Synthesis and selective G-quadruplex stabilizing properties
Macrocyclic hexaoxazoles having one or two lysinyl side chains in which the terminal nitrogen is either a primary amine, N,N-dimethylamine, or an acetamide have been synthesized. Sodium ion has been found to be beneficial to the macrocyclization step by acting as a template around which the linear polyoxazole can organize. Each of the targeted compounds selectivity stabilizes G-quadruplex versus duplex DNA. Compounds with one valine and one lysine residue display the best combination of G-quadruplex stabilizing ability with no detectable stabilization of duplex DNA.
Rzuczek, Suzanne G.,Pilch, Daniel S.,LaVoie, Edmond J.,Rice, Joseph E.
p. 913 - 917
(2008/12/23)
MULTI-COLOR TIME RESOLVED FLUOROPHORES BASED ON MACROCYCLIC LANTHANIDE COMPLEXES
The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds incorporate hydroxy-isophthalamide moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability. These characteristics distinguish them from known, open- structured ligands.
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Page/Page column 72-73
(2008/12/07)
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