TELOMERASE INHIBITORS – OLIGONUCLEOTIDE PHOSPHORAMIDATES AS POTENTIAL THERAPEUTIC AGENTS
- 31 March 2001
- journal article
- Published by Taylor & Francis in Nucleosides, Nucleotides and Nucleic Acids
- Vol. 20 (4-7) , 401-410
- https://doi.org/10.1081/ncn-100002314
Abstract
We have designed, synthesized, and evaluated using physical, chemical and biochemical assays various oligonucleotide N3′ → P5′ phosphoramidates, as potential telomerase inhibitors. Among the prepared compounds were 2′-deoxy, 2′-hydroxy, 2′-methoxy, 2′-ribo-fluoro, and 2′-arabino-fluoro oligonucleotide phosphoramidates, as well as novel N3′ → P5′ thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.Keywords
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