Stable and selective formation of Hoogsteen-type triplexes and duplexes using twisted intercalating nucleic acids (TINA) and process for the preparation of TINA

摘要

Provided is a flexible basestacking monomer with the general structure X - L - I1 - C - I2 wherein X is a backbone monomer unit of an oligonucleotide or an oligonucleotide analogue, or PNA, or PNA analogues, and wherein X comprises alkylenediol, L is a linker comprising an alkyl chain, an oxaalkyl chain, an azaalkyl chain, a thiaalkyl chain, carboxamide group, a thiocarboxamide group, a sulphonamide group or combinations thereof and comprises between 0-60 atoms, I1 is a monocyclic or a polycyclic aromatic ringsystem selected from the group consisting of benzene, naphthalene, azulene and bicyclic heteroaromatic ring systems, C is a conjugator selected from the group of alkyl of 1 to 12 carbons, alkeny of 2 to 12 carbons, alkynyl of 2 to 25 carbons or diazo or combinations thereof with a length of no more than 25 carbons or/and nitrogen atoms, I2 is selected from the group of bicyclic aromatic ringsystems, tricyclic aromatic ringsystems, tetracyclic aromatic ringsystems, pentacyclic aromatic ringsystems and heteroaromatic analogues thereof and such compounds with substitutions thereof. The composition can be used as a medicament targeted to specific genes or RNAs depending on the sequence of the included oligonucleotide.