INTRODUCTION OF A LIPOPHILIC THIOETHER TETHER IN THE MINOR-GROOVE OF NUCLEIC-ACIDS FOR ANTISENSE APPLICATIONS

被引:27
作者
MANOHARAN, M
JOHNSON, LK
TIVEL, KL
SPRINGER, RH
COOK, PD
机构
[1] Department of Medicinal Chemistry, Isis Pharmaceuticals, Carlsbad, CA 92008
关键词
D O I
10.1016/S0960-894X(01)80760-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A 2'-O-hexylthiotrityl adenosine phosphoramidite has been synthesized and incorporated into oligonucleotide phosphodiesters and phosphorothioates. This tether has potential antisense applications, offers a convenient nucleophile for conjugation of various moieties that would reside in the minor groove, and may form novel tertiary structures.
引用
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页码:2765 / 2770
页数:6
相关论文
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