Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines
Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines
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DOI：
10.1016/j.bmc.2010.02.035
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发表时间：
2010-04-01
影响因子：
3.5
通讯作者：
O'Neill, Paul M.
中科院分区：
文献类型：
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作者：
Chadwick, James;Jones, Michael;O'Neill, Paul M.
已经制备了一系列青蒿素-亚精胺缀合物，旨在利用癌细胞中发现的上调多胺转运蛋白。这些缀合物针对人类早幼粒细胞白血病 HL-60 细胞和氯喹敏感的 3D7 恶性疟原虫进行了评估，其中几种缀合物显示出有希望的抗癌和抗疟活性。尽管这种基于载体的方法存在一些明显的局限性，但已鉴定出许多高效 Boc 保护的类似物，其抗疟疾寄生虫的活性低至 0.21 nM。 (C) 2010 Elsevier Ltd. 保留所有权利。
A series of artemisinin-spermidine conjugates designed to utilise the upregulated polyamine transporter found in cancer cells have been prepared. These conjugates were evaluated against human promyelocytic leukaemia HL-60 cells and chloroquine-sensitive 3D7 Plasmodium falciparum and several show promising anticancer and antimalarial activity. Although some limitations in this vector-based approach are apparent, a number of high potency Boc-protected analogues were identified with activity against malaria parasites as low as 0.21 nM. (C) 2010 Elsevier Ltd. All rights reserved.