Isobrassinin and its analogues:: Novel types of antiproliferative agents

被引：36

作者：

Csomos, Peter

Zupko, Istvan

Rethy, Borbala

Fodor, Lajos

Falkay, George

Bernath, Gadbor

机构：

[1] Univ Szeged, Inst Pharmaceut Chem, H-6701 Szeged, Hungary

[2] Hungarian Acad Sci, Res Grp Heterocycl Chem, H-6701 Szeged, Hungary

[3] Cty Hosp, Cent Lab, H-5701 Gyula, Hungary

[4] Univ Szeged, Dept Pharmacodynam & Biopharm, H-6701 Szeged, Hungary

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 24期

基金：

匈牙利科学研究基金会;

关键词：

2-aminomethylindole; dithiocarbamate; thiazino[5,6-b]indole; antitumour activity;

D O I：

10.1016/j.bmcl.2006.09.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Isobrassinin (2-(S-methyidithiocarbamoylaminomethyl)indole (7a), a regioisomer of the cruciferous phytoalexin brassinin (1), exerted marked antiproliferative effects on the HeLa, A431 and MCF7 cell lines (> 78.6% inhibition at 30 mu M). For structure-activity relationships, further analogues were synthesized. The highest cytotoxic effect was displayed by 2-phenylimino-1,3-thiazino[5.6-b]indole (10) (10 mu M, 76.8%-HeLa and 46.3% -MCF7). The effect of the natural phytoalexin brassinin was also determined. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：6273 / 6276

页数：4

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