Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

被引：39

作者：

Fan, YH

Chen, H

Natarajan, A

Guo, YH

Harbinski, F

Iyasere, J

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 / 10期

关键词：

troglitazone; intracellular calcium; thiazolidinediones;

D O I：

10.1016/j.bmcl.2004.02.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：2547 / 2550

页数：4

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