Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction

被引：22

作者：

Feng, Tzu-Shean ^{[1
,2
]}

Guantai, Eric M. ^{[3
]}

Nell, Margo J. ^{[4
]}

van Rensburg, Constance E. J. ^{[4
]}

Hoppe, Heinrich C. ^{[2
]}

Chibale, Kelly ^{[1
,5
]}

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

[2] Univ Cape Town, Div Pharmacol, ZA-7925 Observatory, South Africa

[3] Univ Nairobi, Div Pharmacol, Sch Pharm, Nairobi, Kenya

[4] Univ Pretoria, Dept Pharmacol, ZA-0028 Hatfield, South Africa

[5] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 10期

基金：

新加坡国家研究基金会; 英国医学研究理事会;

关键词：

Anticancer; Antiplasmodial; Aza-Michael addition reaction; Chloroquinoline; Dihydroartemisinin; ANTIMALARIAL ARTESUNATE; FALCIPARUM-MALARIA; IN-VITRO; ARTEMISININ; DRUGS; 4-AMINOQUINOLINES; CHLOROQUINE; DERIVATIVES; INHIBITION; RESISTANCE;

D O I：

10.1016/j.bmcl.2011.03.090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of dihydroartemisinin derivatives were synthesized via an aza-Michael addition reaction to a dihydroartemisinin-based acrylate and were evaluated for antiplasmodial and antitumor activity. The target compounds showed excellent antiplasmodial activity, with dihydroartemisinin derivatives 5, 7, 9 and 13 exhibiting IC50 values of <= 10 nM against both D10 and Dd2 strains of Plasmodium falciparum. Derivative 4d was the most active against the HeLa cancer cell line, with an IC50 of 0.37 mu M and the highest tumor specificity. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2882 / 2886

页数：5

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