| abstract |
Disclosed are oligonucleoside boranophosphates, or salts thereof, comprising a chain of natural or modified ribonucleotides or deoxyribonucleotides, containing at least one boronated internucleotide phospodiester linkage of formula (III), wherein W is selected from the group consisting of =O, =S, -OPr, and -SPr where Pr is a base-labile protecting group. X is selected from the group consisting of -BH3?, -BH2?R1?, -BHR1?R2? and -BR1?R2?R3?. R1? is selected from the group consisting of -R4?, -COOH, -COOR4?, -CONHR4?, -CON(R4?)2?, -CN?+R4?, -CN, carboxycholesteryl and carboxybenzyl, wherein R4? is C1 to C18 alkyl. R2? is selected from the group consisting of -R5?, -COOH, COOR5?, -CONHR5?, -CON(R5?)2?, -CN?+R5?, -CN, carboxy- cholesteryl and carboxybenzyl, wherein R5? is C1 to C18 alkyl. R3? is selected from the group consisting of C1 to C3 alkyl. Most preferably, X is -BH3? and W is =O. Compounds of formula (III) are useful as antisense agents and probes in molecular biology, and have pharmacological activities including anti-inflammatory, antihyperlipidemic, and antineoplastic activity. |