Solid-Phase Synthesis of Phosphate/Boranophosphate Chimeric DNAs Using the H-Phosphonate-H-Boranophosphonate Method.
J Org Chem
; 84(23): 15032-15041, 2019 12 06.
Article
em En
| MEDLINE
| ID: mdl-31657569
ABSTRACT
Boranophosphate (PB) DNAs are promising antisense oligonucleotide candidates because of their attractive features, such as high nuclease resistance and low toxicity. However, a full boranophosphate backbone modification to antisense DNAs causes reduced duplex formation with complementary RNAs and reduced antisense activity. In this study, an efficient solid-phase synthesis of phosphate/boranophosphate (PO/PB) chimeric DNA was achieved by the combination of the H-phosphonate and H-boranophosphonate methods. The physiological and biological properties of the synthesized PO/PB chimeric DNAs were also evaluated. The strategy employed herein can facilitate the design and synthesis of PO/PB chimeric DNAs containing site-specific boranophosphate modifications.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fosfatos
/
Boranos
/
DNA
/
Técnicas de Síntese em Fase Sólida
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article