2'-修饰的2-硫代胸苷寡核苷酸
2'-modified-2-thiothymidine oligonucleotides.
作者信息
Rajeev Kallanthottathil G, Prakash Thazha P, Manoharan Muthiah
机构信息
Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc., Carlsbad, California 92008, USA.
出版信息
Org Lett. 2003 Aug 21;5(17):3005-8. doi: 10.1021/ol0348607.
[reaction: see text] Oligonucleotides with novel modifications, 2'-O-[2-(methoxy)ethyl]-2-thiothymidine and 2'-deoxy-2'-fluoro-2-thiothymidine, have been synthesized. These modified oligonucleotides exhibited very high thermal stability when hybridized with complementary RNA. 2-O-(2-Methoxy)ethyl-2-thiothymidine modified oligonucleotide phosphodiesters showed enhanced resistance toward nucleases (t(1/2) > 24 h), but 2'-deoxy-2'-fluoro-2-thiothymidine modified oligonucleotide phosphodiesters showed limited stability to nucleotytic degradation.
[反应：见正文] 已合成具有新型修饰的寡核苷酸，即2'-O-[2-(甲氧基)乙基]-2-硫代胸苷和2'-脱氧-2'-氟-2-硫代胸苷。这些修饰的寡核苷酸与互补RNA杂交时表现出非常高的热稳定性。2-O-(2-甲氧基)乙基-2-硫代胸苷修饰的寡核苷酸磷酸二酯对核酸酶的抗性增强（半衰期>24小时），但2'-脱氧-2'-氟-2-硫代胸苷修饰的寡核苷酸磷酸二酯对核苷酸降解的稳定性有限。
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