Telomerase inhibitors--oligonucleotide phosphoramidates as potential therapeutic agents.

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.

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@article{Gryaznov2001TelomeraseIP, title={Telomerase inhibitors--oligonucleotide phosphoramidates as potential therapeutic agents.}, author={S Gryaznov and K Pongracz and T Matray and R Schultz and R Pruzan and J Aimi and A Chin and C Harley and B Shea-Herbert and J Shay and Y Oshima and A Asai and Y Yamashita}, journal={Nucleosides, nucleotides & nucleic acids}, year={2001}, volume={20 4-7}, pages={401-10} }