Design, synthesis and antiproliferative activity of tripentones: A new series of antitubulin agents

被引：45
|
作者：
Lisowski, V
Enguehard, C
Lancelot, JC
Caignard, DH
Lambel, S
Leonce, S
Pierre, A
Atassi, G
Renard, P
Rault, S
机构：
[1] UFR Sci Pharmaceut, Ctr Etud & Rech Medicament Normandie, F-14032 Caen, France
[2] UFR Sci Pharmaceut, F-37200 Tours, France
[3] ADIR, F-92415 Courbevoie, France
[4] Inst Rech Servier, F-92150 Suresnes, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期
关键词：
D O I：
10.1016/S0960-894X(01)00403-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-activity relationship studies of a new series of tripentones (thieno[2.3-h]pyrrolizin-8-ones), led us to prepare several derivatives with antiproliferative activities. The most promising 3-(3-hydroxy-4-methoxyphenyl)thieno[2.3-b]pyrrolizin-8-one 20 (leukemia L1210. IC50= 15 nM) was shown to be a potent inhibitor of tubulin polymerization. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2205 / 2208
页数：4
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