Synthesis and biological evaluation of analogues of the anti-tumor alkaloid naamidine A

被引：30

作者：

Aberle, Nicholas

Catime, Jenny

Nice, Edouard C.

Watson, Keith G.

机构：

[1] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3050, Australia

[2] Univ Melbourne, Dept Med Biol, Parkville, Vic 3010, Australia

[3] Royal Melbourne Hosp, Ludwig Inst Canc Res, Parkville, Vic 3050, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 13期

关键词：

naamidine A; structure-activity relationship; 2-aminoimidazole; 2-aminothiazole; anti-tumor; dehydrohydantoin;

D O I：

10.1016/j.bmcl.2007.04.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A small series of derivatives of the alkaloid naamidine A was synthesized and tested in vitro for their ability to inhibit mitogenesis in BaF/ERX cells. Replacement of the imidazole core with a thiazole was found to have only a minor effect on potency, and the 4-metlioxybenzyl substituent of the natural product was shown to be unnecessary for activity. (c) 2007 Elsevier Ltd. All rights reserved.

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页码：3741 / 3744

页数：4

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