کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365490 981562 2006 12 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antisense oligonucleotides: Efficient synthesis of 2′-O-methoxyethyl phosphorothioate oligonucleotides using 4,5-dicyanoimidazole. Are these oligonucleotides comparable to those synthesized using 1H-tetrazole as coupling activator?
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Antisense oligonucleotides: Efficient synthesis of 2′-O-methoxyethyl phosphorothioate oligonucleotides using 4,5-dicyanoimidazole. Are these oligonucleotides comparable to those synthesized using 1H-tetrazole as coupling activator?
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 14, 15 July 2006, Pages 5049–5060
نویسندگان
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