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

页码：2205 / 2208

页数：4

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