Tubulin-polymerization inhibitors derived from thalidomide
Tubulin-polymerization inhibitors derived from thalidomide
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DOI：
10.1016/j.bmcl.2004.10.072
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发表时间：
2005-01-17
影响因子：
2.7
通讯作者：
Kobayashi, H
中科院分区：
文献类型：
--
作者：
Inatsuki, S;Noguchi, T;Kobayashi, H
2-（2，6-Diisopropylphenyl）-5-hydroxy-1H-isoindole-1，3-dione（5 HPP-33）是我们在对沙利度胺进行结构开发研究时得到的一个化合物，它具有与已知的微管蛋白聚合抑制剂rhizoxin和秋水仙碱相当的微管蛋白聚合抑制活性。沙利度胺的主要代谢产物5-羟基沙利度胺在对应于5 HPP-33的位置处具有羟基，也显示出中等抑制活性。(C)2004 Elsevier Ltd.保留所有权利。
2-(2,6-Diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione (5HPP-33), which was obtained during our previous structural development studies on thalidomide, was revealed to possess potent tubulin-polymerization-inhibiting activity, comparable to that of the known tubulin-polymerization inhibitors, rhizoxin and colchicine. A major metabolite of thalidomide, 5-hydroxythalidomide, which possesses a hydroxyl group at the position corresponding to that of 5HPP-33, also showed moderate inhibitory activity. (C) 2004 Elsevier Ltd. All rights reserved.