Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents

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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.

Original languageEnglish (US)
Pages (from-to)401-410
Number of pages10
JournalNucleosides, Nucleotides and Nucleic Acids
Volume20
Issue number4-7
DOIs
StatePublished - Jan 1 2001

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Genetics

Cite this

Gryaznov, S., Pongracz, K., Matray, T., Schultz, R., Pruzan, R., Aimi, J., Chin, A., Harley, C., Shea-Herbert, B., Shay, J., Oshima, Y., Asai, A., & Yamashita, Y. (2001). Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents. Nucleosides, Nucleotides and Nucleic Acids, 20(4-7), 401-410. https://doi.org/10.1081/NCN-100002314