Crucial role of linker portion in acridine-bearing oligonucleotides for highly efficient site-selective RNA scission

Through a series of linkers, 9-amino-2-methoxy-6-nitroacridine and 9-amino-6-chloro-2-methoxyacridine were tethered to the middle of oligonucleotide, and the abilities of these conjugates for site-selective activation of RNA (inducing site-selective scission by Lu(III)) were compared. The RNA-activating ability was strongly dependent on the structures of both acridine and linker. By tethering 9-amino-2-methoxy-6-nitroacridine with a rigid and chiral linker, derived from l-threoninol, quite fast site-selective RNA scission was accomplished.