Endoxifen is a new potent inhibitor of PKC: A potential therapeutic agent for bipolar disorder

被引：34

作者：

Ali, Shoukath M. ^{[1
]}

Ahmad, Ateeq ^{[1
]}

Shahabuddin, Syed ^{[1
]}

Ahmad, Moghis U. ^{[1
]}

Sheikh, Saifuddin ^{[1
]}

Ahmad, Imran ^{[1
]}

机构：

[1] Jina Pharmaceut Inc, Libertyville, IL 60048 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期

关键词：

Endoxifen; PKC; Bipolar disorder; Chemical synthesis; KINASE-C ACTIVITY; TAMOXIFEN; MANIA;

D O I：

10.1016/j.bmcl.2010.02.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen. (C) 2010 Elsevier Ltd. All rights reserved.

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收藏

页码：2665 / 2667

页数：3

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