公开(公告)号：US20060167106A1

公开(公告)日：2006-07-27

申请号：US11283570

申请日：2005-11-18

申请人： Mei Zhang ,  Andras Ladanyi

发明人： Mei Zhang ,  Andras Ladanyi

IPC分类号： A61K31/16 ,  C07C327/40

CPC分类号： G01N33/5035 ,  A61K31/00 ,  A61K31/16 ,  A61K31/165 ,  A61K39/02 ,  A61K45/06 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/6875 ,  G01N2800/382 ,  A61K2300/00

摘要： The present invention relates to compounds, and methods utilizing compounds, which exhibit one or more of the following properties: i) disrupts organization of an actin cytoskeleton of a cell; ii) disrupts organization of a microtubule network of a cell; iii) induces accumulation of tubulin at centrosomes but does not induce accumulation of tubulin in a nucleus of a cell; iv) induces accumulation of tubulin at centrosomes at a concentration of 500 nM or less within four hours; v) induces accumulation of Hsp70 and has weak-to-moderate proteasome inhibitory activity; and vi) does not have proteasome inhibitory activity when assayed on purified proteasomes.

摘要翻译： 本发明涉及化合物和利用化合物的方法，其具有以下一个或多个性质：i）破坏细胞的肌动蛋白细胞骨架的组织; ii）破坏细胞微管网络的组织; iii）诱导微管蛋白在中心体的积累，但不诱导微管蛋白在细胞核中的积累; iv）在四小时内以500nM或更小的浓度诱导中心体上的微管蛋白积累; v）诱导Hsp70的积累并具有弱至中度的蛋白酶体抑制活性; 和vi）在纯化的蛋白酶体上测定时不具有蛋白酶体抑制活性。