Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents

Authors
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
Citation
S. Gryaznov et al., Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents, NUCLEOS NUC, 20(4-7), 2001, pp. 401-410
Citations number
20
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
15257770 → ACNP
Volume
20
Issue
4-7
Year of publication
2001
Pages
401 - 410
Database
ISI
SICI code
1525-7770(2001)20:4-7<401:TI-OPA>2.0.ZU;2-9
Abstract
We have designed, synthesized, and evaluated using physical, chemical and b iochemical 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 oligonucleo tide phosphoramidates, as well as novel N3' --> P5' thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity wi th IC50 values in the sub-nM to pM concentration range.