| abstract |
OLIGORIBONUCLEOSIDE AND OLIGODEOXYRIBONUCLEOSIDE BORANOPHOSPHATES 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 the formula: (III) 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, -BH2R1, -BHR1R2 and -BR1R2R3. 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 -R3, -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. |