Antileukemic activity of aminoparthenolide analogs

被引：86

作者：

Nasim, Shama ^{[1
]}

Crooks, Peter A. ^{[1
]}

机构：

[1] Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

sesquiterpene lactones; parthenolide analogs; antileukemic activity;

D O I：

10.1016/j.bmcl.2008.06.050

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aminoparthenolide analogs have been synthesized through a diastereoselective conjugate addition of several primary and secondary amines to the alpha-methylene-gamma-butyrolactone function of the very lipophilic sesquiterpene lactone, parthenolide. Seventeen of the above amines derivatives were evaluated in a full panel of 60 cancer cell lines for anticancer activity. Compound 12, derived from tyramine, was found to be cytostatic as well as cytotoxic toward acute lymphoblastic leukemia cells (ALL, CCRF-CEM) at nanomolar concentrations, while the (R)-(1,2,3,4-tetrahydro-1-naphthyl)amino derivative 9 was found to be cytostatic toward human anaplastic large T-cell lymphoma (SR) cells at concentrations below 10 nM. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3870 / 3873

页数：4

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