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Research article - Peer-reviewed, 2004

Synthesis, physicochemical and biochemical studies of 1',2'-oxetane constrained adenosine and guanosine modified oligonucleotides, and their comparison with those of the corresponding cytidine and thymidine analogues

Pradeepkumar PI, Cheruku P, Plashkevych O, Acharya P, Gohil S, Chattopadhyaya J


We have earlier reported the synthesis and antisense properties of the conformationally constrained oxetane-C and -T containing oligonucleotides, which have shown effective down-regulation of the proto-oncogene c-myb mRNA in the K562 human leukemia cells. Here we report on the straightforward syntheses of the oxetane-A and oxetane-G nucleosides as well as their incorporations into antisense oligonucleotides (AONs), and compare their structural and antisense properties with those of the T and C modified AONs (including the thermostability and RNase H recruitment capability of the AON/RNA hybrid duplex by Michaelis-Menten kinetic analyses, their resistance in the human serum, as well as in the presence of exo and endonucleases)

Published in

Journal of the American Chemical Society
2004, volume: 126, number: 37, pages: 11484-11499

Authors' information

Swedish University of Agricultural Sciences, Department of Chemistry
Acharya, P
Chattopadhyaya, J
Cheruku, P
Plashkevych, O
Pradeepkumar, P I

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