Synthesis and biological evaluation of thiazolidine-2,4-dione and 2,4-thione derivatives as inhibitors of translation initiation

被引：49

作者：

Chen, H

Fan, YH

Natarajan, A

Guo, YH

Iyasere, J

Harbinski, F

Luus, L

Christ, W

Aktas, H

Halperin, JA ^{[1
]}

机构：

[1] Harvard Univ, Sch Med, Lab Translat Res, Cambridge, MA 02139 USA

[2] Brigham & Womens Hosp, Dept Med, Boston, MA 02115 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 21期

关键词：

translation initiation inhibitors; cancer therapy; thiazolidine-2,4-thione; thiazolidine-2,4-dione;

D O I：

10.1016/j.bmcl.2004.08.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an effort to generate novel translation initiation inhibitors for cancer therapy, a series of 2'-benzyloxy-5'-substituted-5-benzylidene-thiazolidine-2,4-thione and dione derivatives was synthesized and evaluated for activity in translation initiation specific assays. Several candidates of the 5-benzylidene-thiazolidine-2,4-diones (3c, 3d, and 3f) and -thiones (2b, 2e, and 2j), inhibit cell growth with low muM GI(50) mediated by inhibition of translation initiation, which involves partial depletion of intracellular Ca2+ stores and strong phosphorylation of eIF2alpha. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：5401 / 5405

页数：5

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