Identification of novel and improved antimitotic agents derived from noscapine

被引：58

作者：

Anderson, JT ^{[1
]}

Ting, AE ^{[1
]}

Boozer, S ^{[1
]}

Brunden, KR ^{[1
]}

Crumrine, C ^{[1
]}

Danzig, J ^{[1
]}

Dent, T ^{[1
]}

Faga, L ^{[1
]}

Harrington, JJ ^{[1
]}

Hodnick, WF ^{[1
]}

Murphy, SM ^{[1
]}

Pawlowski, G ^{[1
]}

Perry, R ^{[1
]}

Raber, A ^{[1
]}

Rundlett, SE ^{[1
]}

Stricker-Krongrad, A ^{[1
]}

Wang, JM ^{[1
]}

Bennani, YL ^{[1
]}

机构：

[1] Athersys Inc, Cleveland, OH 44115 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 23期

关键词：

D O I：

10.1021/jm050674q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogues of the natural product noscapine were synthesized and their potential as antitumor agents evaluated. The discovery of a novel regioselective 0-demethylation facilitated the synthesis of the potent aniline 6, which arrests mammalian cells in the G2/M phase of the cell cycle at 0.1 mu M and also affects tubulin polymerization. Aniline 6 is orally bioavailable and is 250-fold more potent than noscapine in reducing cell proliferation in rapidly dividing cells.

引用

页码：7096 / 7098

页数：3

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