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一系列含有取代查尔酮的新型双氢青蒿素衍生物的合成,其对白血病细胞具有更强的细胞毒性作用。

Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.

作者信息

Yang Xuelin, Wang Wei, Tan Jun, Song Dandan, Li Ming, Liu Dan, Jing Yongkui, Zhao Linxiang

机构信息

Shenyang Pharmaceutical University, Shenyang 110016, PR China.

出版信息

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4385-8. doi: 10.1016/j.bmcl.2009.05.076. Epub 2009 May 27.

Abstract

Fifteen dihydroartemisinin derivatives containing a substituted chalcone linked by either ether or ester were synthesized and investigated for their cytotoxicity in human leukemia HL-60 and mouse lymphoma P388 cells. These derivatives have greater antiproliferative and cytotoxic effects in both cell lines than dihydroartemisinin. Dihydroartemisinin chalcones linked by ether are more cytotoxic than dihydroartemisinin chalcones linked by ester with apoptosis induction abilities.

摘要

合成了15种含有通过醚键或酯键连接的取代查尔酮的双氢青蒿素衍生物,并研究了它们对人白血病HL-60细胞和小鼠淋巴瘤P388细胞的细胞毒性。这些衍生物在两种细胞系中均比双氢青蒿素具有更强的抗增殖和细胞毒性作用。通过醚键连接的双氢青蒿素查尔酮比通过酯键连接的双氢青蒿素查尔酮具有更强的细胞毒性和诱导凋亡能力。

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