Introduction of a lipophilic thioether tether in the minor groove of nucleic acids for antisense applications |
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| Authors: | Muthiah Manoharan Laura K Johnson Kathleen L Tivel Robert H Springer PDan Cook |
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| Institution: | Department of Medicinal Chemistry, Isis Pharmaceuticals, 2280 Faraday Ave, Carlsbad CA 92008 U.S.A. |
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| Abstract: | 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. |
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