TY - JOUR
T1 - Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents
AU - Gryaznov, S.
AU - Pongracz, K.
AU - Matray, T.
AU - Schultz, R.
AU - Pruzan, R.
AU - Aimi, J.
AU - Chin, A.
AU - Harley, C.
AU - Shea-Herbert, B.
AU - Shay, J.
AU - Oshima, Y.
AU - Asai, A.
AU - Yamashita, Y.
PY - 2001
Y1 - 2001
N2 - 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.
AB - 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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U2 - 10.1081/NCN-100002314
DO - 10.1081/NCN-100002314
M3 - Article
C2 - 11563055
AN - SCOPUS:0034839552
SN - 1525-7770
VL - 20
SP - 401
EP - 410
JO - Nucleosides, Nucleotides and Nucleic Acids
JF - Nucleosides, Nucleotides and Nucleic Acids
IS - 4-7
ER -