Telomerase inhibitors - Oligonucleotide phosphoramidates as potential therapeutic agents

被引：64

作者：

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

机构：

[1] Geron Corp, Menlo Pk, CA 94025 USA

[2] UTSW Med Ctr, Houston, TX USA

[3] Kyowa Hakko Kogyo Co Ltd, Tokyo, Japan

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2001年 / 20卷 / 4-7期

关键词：

D O I：

10.1081/NCN-100002314

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

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.

引用

收藏

页码：401 / 410

页数：10

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