کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365490 | 981562 | 2006 | 12 صفحه PDF | دانلود رایگان |

Multiple 2′-O-methoxyethyl modified phosphorothioate oligonucleotides of 18–20-mer in length were synthesized at various scales using 4,5-dicyanoimidazole (DCI) as coupling activator. Extensive synthetic, analytical (using ion-pair LC–MS), and in vivo pharmacological, toxicological studies showed that oligonucleotides made with DCI and 1H-tetrazole are chemically and biologically equivalent. This extensive study will help the oligonucleotide therapeutic industry to move from using a potentially explosive activator (1H-tetrazole) to a safe activator (DCI).
Multiple 2′-O-methoxyethyl modified phosphorothioate oligonucleotides of 18–20-mer in length were synthesized at various scales using 4,5-dicyanoimidazole (DCI) as coupling activator. Extensive synthetic, analytical (using ion-pair LC–MS), and in vivo pharmacological, toxicological studies showed that oligonucleotides made with DCI and 1H-tetrazole are chemically and biologically equivalent. This extensive study will help the oligonucleotide therapeutic industry to move from using a potentially explosive activator (1H-tetrazole) to a safe activator (DCI).Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 14, 15 July 2006, Pages 5049–5060