Preparation and properties of a new type of acyclic, achiral nucleoside analogue |
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Authors: | Boesen Thomas Sejer Pedersen Daniel Jensen Jacob Munck Michael T Nielsen Brian M Petersen Asger B Henriksen Ulla Dahl Britta M Dahl Otto |
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Institution: | Department of Chemistry, University of Copenhagen, The H. C. Orsted Institute, Copenhagen, Denmark. |
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Abstract: | Preparation of the nucleoside analogues 1 and incorporation of 1, B = T, in deoxyribooligonucleotides by the phosphoramidite method is described. A two-step deprotection procedure was developed to reduce cleavage of the modified allylic unit. The binding properties of the modified oligonucleotides towards complementary DNA and RNA has been evaluated by Tm measurements showing a deltaTm of -2 to -6.5 degrees C per modification. An oligonucleotide with two modifications at the 3'-end showed considerable resistance towards cleavage by a 3'-exonuclease. No antiviral activity against HIV-1 or HSV-1 was found for 1, B = G or T, or for any of the trihydroxy derivatives 5. |
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